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2,4-dinitrophenyl S-glutathione/in + ATP + H2O
2,4-dinitrophenyl S-glutathione/out + ADP + H2O
-
-
-
?
3,6-bis(dimethylamino)-9-phenyl-selenoxanthylium bromide/in + ATP + H2O
3,6-bis(dimethylamino)-9-phenyl-selenoxanthylium bromide/out + ADP + phosphate
-
-
-
-
?
3alpha-sulfatolithocholyltaurine/in + ATP + H2O
3alpha-sulfatolithocholyltaurine/out + ADP + phosphate
-
-
-
?
6-mercaptopurine/in + ATP + H2O
6-mercaptopurine/out + ADP + phosphate
-
-
-
?
8-aza-ATP + H2O + 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole/in
8-aza-ADP + phosphate + 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole/out
-
8-aza-ATP is a fairly good substrate of BmrA
-
-
?
8-azido-ATP + H2O
? + phosphate
-
-
-
-
?
8-azido-ATP + H2O + xenobiotic/in
8-azido-ADP + phosphate + xenobiotic/out
-
-
-
-
?
9-(2-phosphonylmethoxyethyl)adenine/in + ATP + H2O
9-(2-phosphonylmethoxyethyl)adenine/out + ADP + phosphate
-
-
-
?
aflatoxin B1-epoxide-GSH conjugate/in + ATP + H2O
aflatoxin B1-epoxide-GSH conjugate/out + ADP + phosphate
-
-
-
?
aflatoxin B1/in + ATP + H2O
aflatoxin B1/out + ADP + phosphate
ATP + H2O
ADP + phosphate
ATP + H2O + 1,13-bis[4'-(4H-chromen-4-on-2-yl)phenyl]-N-(benzyl)-1,4,10,13-tetraoxa-7-azatridecane/in
ADP + phosphate + 1,13-bis[4'-(4H-chromen-4-on-2-yl)phenyl]-N-(benzyl)-1,4,10,13-tetraoxa-7-azatridecane/out
-
-
-
-
?
ATP + H2O + 17beta-estradiol 17-(beta-D-glucuronide)/in
ADP + phosphate + 17beta-estradiol 17-(beta-D-glucuronide)/out
ATP + H2O + 17beta-glucuronosyl oestradiol/in
ADP + phosphate + 17beta-glucuronosyl oestradiol/out
-
-
-
-
?
ATP + H2O + 2',3'-dideoxycytidine/in
ADP + phosphate + 2',3'-dideoxycytidine/out
-
-
-
-
?
ATP + H2O + 2',7'-bis(carboxyethyl)-5(6)-carboxyfluorescein/in
ADP + phosphate + 2',7'-bis(carboxyethyl)-5(6)-carboxyfluorescein/out
-
-
-
-
?
ATP + H2O + 2',7'-bis-(2-carboxyethyl)-5,6-carboxylfluoresceinacetoxymethyl ester/in
ADP + phosphate + 2',7'-bis-(2-carboxyethyl)-5,6-carboxylfluoresceinacetoxymethyl ester/out
ATP + H2O + 2',7'-bis-(3-carboxyethyl)-5-carboxyfluorescein/in
ADP + phosphate + 2',7'-bis-(3-carboxyethyl)-5-carboxyfluorescein/out
-
fluorescent substrate
-
-
?
ATP + H2O + 2',7'-bis-(3-carboxyethyl)-6-carboxyfluorescein/in
ADP + phosphate + 2',7'-bis-(3-carboxyethyl)-6-carboxyfluorescein/out
-
fluorescent substrate
-
-
?
ATP + H2O + 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole/in
ADP + phosphate + 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole/out
ATP + H2O + 2,3,5-triphenylterazolium chloride[side 1]
ADP + phosphate + 2,3,5-triphenylterazolium chloride[side 2]
ATP + H2O + 2,4-dinitrophenyl-S-glutathione[side 1]
ADP + phosphate + 2,4-dinitrophenyl-S-glutathione[side 2]
ATP + H2O + 2,5-dimethoxy-4-iodoamphetamine/in
ADP + phosphate + 2,5-dimethoxy-4-iodoamphetamine/out
-
-
-
-
?
ATP + H2O + 2,7-bis-(2-carboxyethyl)-5-(and-6)-carboxyfluorescein acetoxymethyl ester[side 1]
ADP + phosphate + 2,7-bis-(2-carboxyethyl)-5-(and-6)-carboxyfluorescein acetoxymethyl ester[side 2]
-
-
-
-
?
ATP + H2O + 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine[side 1]
ADP + phosphate + 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine[side 2]
ATP + H2O + 3,3'-dihexyloxacarbocyanine iodide/in
ADP + phosphate + 3,3'-dihexyloxacarbocyanine iodide/out
ATP + H2O + 3,4-methylenedioxy-alpha-ethylphenethylamine/in
ADP + phosphate + 3,4-methylenedioxy-alpha-ethylphenethylamine/out
-
-
-
-
?
ATP + H2O + 4-(2-aminoethyl)benzenesulfonylfluoride/in
ADP + phosphate + 4-(2-aminoethyl)benzenesulfonylfluoride/out
-
-
-
-
?
ATP + H2O + 4-aminohippurate[side 1]
ADP + phosphate + 4-aminohippurate[side 2]
substrate for MPR2
-
-
?
ATP + H2O + 4-aminohippuric acid/in
ADP + phosphate + 4-aminohippuric acid/out
-
-
-
-
?
ATP + H2O + 4-N-(2'-methoxystyryl)-thiosemicarbazone/in
ADP + phosphate + 4-N-(2'-methoxystyryl)-thiosemicarbazone/out
ATP + H2O + 4-nitroquinoline-1-oxide/in
ADP + phosphate + 4-nitroquinoline-1-oxide/out
-
substrate for Snq2p
-
-
?
ATP + H2O + 5-(glutathione-S-yl)-N-methyl-alpha-methyldopamine/in
ADP + phosphate + 5-(glutathione-S-yl)-N-methyl-alpha-methyldopamine/out
-
-
-
-
?
ATP + H2O + 5-fluorouracil[side 1]
ADP + phosphate + 5-fluorouracil[side 2]
ATP + H2O + 6-thioguanine[side 1]
ADP + phosphate + 6-thioguanine[side 2]
substrate for ABCC4
-
-
?
ATP + H2O + 7-aminoactinomycin D/in
ADP + phosphate + 7-aminoactinomycin D/out
-
-
-
-
?
ATP + H2O + 9-hydroxyrisperidone/in
ADP + phosphate + 9-hydroxyrisperidone/out
ATP + H2O + acitretin/in
ADP + phosphate + acitretin/out
-
-
-
-
?
ATP + H2O + acridine orange[side 1]
ADP + phosphate + acridine orange[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + acriflavine [side 1]
ADP + phosphate + acriflavine[side 2]
ATP + H2O + actinomycin D/in
ADP + phosphate + actinomycin D/out
-
-
-
?
ATP + H2O + actinomycin D[side 1]
ADP + phosphate + actinomycin D[side 2]
ATP + H2O + acyclovir/in
ADP + phosphate + acyclovir/out
-
-
-
-
?
ATP + H2O + adefovir/in
ADP + phosphate + adefovir/out
-
-
-
-
?
ATP + H2O + adevovir[side 1]
ADP + phosphate + adevovir[side 2]
substrate for MPR2
-
-
?
ATP + H2O + aflatoxin B[side 1]
ADP + phosphate + aflatoxin B[side 2]
substrate for MRP1
-
-
?
ATP + H2O + allopurinol/in
ADP + phosphate + allopurinol/out
-
-
-
-
?
ATP + H2O + amiodarone[side 1]
ADP + phosphate + amiodarone[side 2]
ATP + H2O + ampicillin[side 1]
ADP + phosphate + ampicillin[side 2]
substrate for MPR2
-
-
?
ATP + H2O + amprenavir[side 1]
ADP + phosphate + amprenavir[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + anisomycin/in
ADP + phosphate + anisomycin/out
ATP + H2O + arsenite[side 1]
ADP + phosphate + arsenite[side 2]
substrate for MRP1
-
-
?
ATP + H2O + asimadoline[side 1]
ADP + phosphate + asimadoline[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + azacytidine[side 1]
ADP + phosphate + azacytidine[side 2]
substrate for ABCC4
-
-
?
ATP + H2O + azidopine[side 1]
ADP + phosphate + azidopine[side 2]
ATP + H2O + azidothymidine[side 1]
ADP + phosphate + azidothymidine[side 2]
substrate for BCRP
-
-
?
ATP + H2O + azithromycin[side 1]
ADP + phosphate + azithromycin[side 2]
substrate for MPR2
-
-
?
ATP + H2O + azole/in
ADP + phosphate + azole/out
-
the ABC multidrug transporter Cdr1p plays a key role in azole resistance
-
-
?
ATP + H2O + BCECF-acetoxymethylester[side 1]
ADP + phosphate + BCECF-acetoxymethylester[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + bepridil[side 1]
ADP + phosphate + bepridil[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + beta-estradiol 17-beta-D-glucuronide/in
ADP + phosphate + beta-estradiol 17-beta-D-glucuronide/out
-
-
-
-
?
ATP + H2O + beta-estradiol/in
ADP + phosphate + beta-estradiol/out
-
-
-
-
?
ATP + H2O + bilirubin[side 1]
ADP + phosphate + bilirubin[side 2]
substrate for MRP1
-
-
?
ATP + H2O + bimatoprost/in
ADP + phosphate + bimatoprost/out
-
-
-
-
?
ATP + H2O + bisantrene[side 1]
ADP + phosphate + bisantrene[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + Bodipy-verapamil/in
ADP + phosphate + Bodipy-verapamil/out
-
-
-
-
?
ATP + H2O + bodipy-vinblastine/in
ADP + phosphate + bodipy-vinblastine/out
-
-
-
-
?
ATP + H2O + buspirone/in
ADP + phosphate + buspirone/out
ATP + H2O + C12E08/in
ADP + phosphate + C12E08/out
-
-
-
?
ATP + H2O + caffeine/in
ADP + phosphate + caffeine/out
-
Snq2p is a more functional transporter of caffeine than Pdr5p in yeast cells
-
-
?
ATP + H2O + calcein acetoxymethylester/in
ADP + phosphate + calcein acetoxymethylester/out
-
-
-
-
?
ATP + H2O + calcein acetoxymethylester[side 1]
ADP + phosphate + calcein acetoxymethylester[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + calcein-acetoxymethylester[side 1]
ADP + phosphate + calcein-acetoxymethylester[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + calcein/in
ADP + phosphate + calcein/out
ATP + H2O + calcein[side 1]
ADP + phosphate + calcein[side 2]
ATP + H2O + calphostin C[side 1]
ADP + phosphate + calphostin C[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + cAMP/in
ADP + phosphate + cAMP/out
-
-
-
-
?
ATP + H2O + carboxydichlorofluorescein/in
ADP + phosphate + carboxydichlorofluorescein/out
-
-
-
-
?
ATP + H2O + cefazolin/in
ADP + phosphate + cefazolin/out
-
-
-
-
?
ATP + H2O + cefmetazole/in
ADP + phosphate + cefmetazole/out
-
-
-
-
?
ATP + H2O + cefodizime[side 1]
ADP + phosphate + cefodizime[side 2]
substrate for MPR2
-
-
?
ATP + H2O + cefoperazone[side 1]
ADP + phosphate + cefoperazone[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + cefotaxime/in
ADP + phosphate + cefotaxime/out
-
-
-
-
?
ATP + H2O + ceftizoxime/in
ADP + phosphate + ceftizoxime/out
-
-
-
-
?
ATP + H2O + ceftriaxone[side 1]
ADP + phosphate + ceftriaxone[side 2]
ATP + H2O + celecoxib/in
ADP + phosphate + celecoxib/out
-
-
-
-
?
ATP + H2O + cerivastatin[side 1]
ADP + phosphate + cerivastatin[side 2]
substrate for BCRP
-
-
?
ATP + H2O + cGMP/in
ADP + phosphate + cGMP/out
-
-
-
-
?
ATP + H2O + chenodeoxycholic acid[side 1]
ADP + phosphate + chenodeoxycholic acid[side 2]
-
-
-
?
ATP + H2O + chenodeoxycholylglycine/in
ADP + phosphate + chenodeoxycholylglycine/out
-
-
-
-
?
ATP + H2O + chenodeoxycholyltaurine/in
ADP + phosphate + chenodeoxycholyltaurine/out
-
-
-
-
?
ATP + H2O + chlorambucil[side 1]
ADP + phosphate + chlorambucil[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + chlorpromazine/in
ADP + phosphate + chlorpromazine/out
ATP + H2O + chlorpromazine[side 1]
ADP + phosphate + chlorpromazine[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + cholate/in
ADP + phosphate + cholate/out
-
-
-
-
?
ATP + H2O + cholesterol/in
ADP + phosphate + cholesterol/out
ATP + H2O + cholesterol[side 1]
ADP + phosphate + cholesterol[side 2]
the enzyme does not catalyze significant cholesterol transport in vivo
-
-
?
ATP + H2O + cholic acid[side 1]
ADP + phosphate + cholic acid[side 2]
-
-
-
?
ATP + H2O + cholylglycine/in
ADP + phosphate + cholylglycine/out
-
-
-
-
?
ATP + H2O + cholytaurine/in
ADP + phosphate + cholytaurine/out
-
-
-
-
?
ATP + H2O + chrysin[side 1]
ADP + phosphate + chrysin[side 2]
substrate for BCRP
-
-
?
ATP + H2O + cidofovir[side 1]
ADP + phosphate + cidofovir[side 2]
substrate for MPR2
-
-
?
ATP + H2O + cimetidine[side 1]
ADP + phosphate + cimetidine[side 2]
ATP + H2O + ciprofloxacin[side 1]
ADP + phosphate + ciprofloxacin[side 2]
ATP + H2O + cisplatin[side 1]
ADP + phosphate + cisplatin[side 2]
substrate for P-glycoprotein and MPR2
-
-
?
ATP + H2O + citalopram/in
ADP + phosphate + citalopram/out
ATP + H2O + clarithromycin[side 1]
ADP + phosphate + clarithromycin[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + clorambucil[side 1]
ADP + phosphate + clorambucil[side 2]
substrate for MRP1
-
-
?
ATP + H2O + clotrimazole/in
ADP + phosphate + clotrimazole/out
ATP + H2O + colchicine/in
ADP + phosphate + colchicine/out
ATP + H2O + colchicine[side 1]
ADP + phosphate + colchicine[side 2]
ATP + H2O + corticosterone/in
ADP + phosphate + corticosterone/out
-
-
-
-
?
ATP + H2O + cyclic guanosine monophosphate/in
ADP + phosphate + cyclic guanosine monophosphate/out
-
-
-
-
?
ATP + H2O + cyclobenzaprine/in
ADP + phosphate + cyclobenzaprine/out
ATP + H2O + cycloheximide /in
ADP + phosphate + cycloheximide /out
-
-
-
-
?
ATP + H2O + cycloheximide/in
ADP + phosphate + cycloheximide/out
ATP + H2O + cycloheximide[side 1]
ADP + phosphate + cycloheximide[side 2]
ATP + H2O + cyclophosphamide[side 1]
ADP + phosphate + cyclophosphamide[side 2]
substrate for MRP1
-
-
?
ATP + H2O + cyclosporin A/in
ADP + phosphate + cyclosporin A/out
ATP + H2O + cyclosporin A[side 1]
ADP + phosphate + cyclosporin A[side 2]
substrate for P-glycoprotein and BCRP
-
-
?
ATP + H2O + cyclosporin H[side 1]
ADP + phosphate + cyclosporin H[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + cyclosporine A/in
ADP + phosphate + cyclosporine A/out
-
-
-
-
?
ATP + H2O + cyclosporine A[side 1]
ADP + phosphate + cyclosporine A [side 2]
-
-
-
?
ATP + H2O + cyclosporine A[side 1]
ADP + phosphate + cyclosporine A[side 2]
ATP + H2O + cyclosporine[side 1]
ADP + phosphate + cyclosporine[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + cytarabine/in
ADP + phosphate + cytarabine/out
-
-
-
-
?
ATP + H2O + cytarabine[side 1]
ADP + phosphate + cytarabine[side 2]
ATP + H2O + darunavir/in
ADP + phosphate + darunavir/out
-
-
-
-
?
ATP + H2O + daunomycin/in
ADP + phosphate + daunomycin/out
ATP + H2O + daunomycin[side 1]
ADP + phosphate + daunomycin[side 2]
-
-
-
?
ATP + H2O + daunorubicin/in
ADP + phosphate + daunorubicin/out
ATP + H2O + daunorubicin[side 1]
ADP + phosphate + daunorubicin[side 2]
ATP + H2O + dehydroepiandrosterone sulfate/in
ADP + phosphate + dehydroepiandrosterone sulfate/out
-
-
-
-
?
ATP + H2O + dehydroepiandrosterone sulfate[side 1]
ADP + phosphate + dehydroepiandrosterone sulfate[side 2]
substrate for MRP1
-
-
?
ATP + H2O + dehydroepiandrosterone-3-sulfate/in
ADP + phosphate + dehydroepiandrosterone-3-sulfate/out
-
-
-
-
?
ATP + H2O + delavirdine[side 1]
ADP + phosphate + delavirdine[side 2]
substrate for BCRP
-
-
?
ATP + H2O + deoxycholic acid[side 1]
ADP + phosphate + deoxycholic acid[side 2]
-
-
-
?
ATP + H2O + deoxycholylglycine/in
ADP + phosphate + deoxycholylglycine/out
-
-
-
-
?
ATP + H2O + deoxycorticosterone/in
ADP + phosphate + deoxycorticosterone/out
-
-
-
-
?
ATP + H2O + dexamethasone/in
ADP + phosphate + dexamethasone/out
-
-
-
-
?
ATP + H2O + diazepam/in
ADP + phosphate + diazepam/out
ATP + H2O + diclofenac/in
ADP + phosphate + diclofenac/out
-
substrate of BCRP, but not of P-gp and MDR1
-
-
?
ATP + H2O + digitonin[side 1]
ADP + phosphate + digitonin[side 2]
-
-
-
?
ATP + H2O + digoxin/in
ADP + phosphate + digoxin/out
-
-
-
-
?
ATP + H2O + digoxin[side 1]
ADP + phosphate + digoxin[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + diltiazem/in
ADP + phosphate + diltiazem/out
ATP + H2O + diltiazem[side 1]
ADP + phosphate + diltiazem[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + dinitrophenyl[side 1]
ADP + phosphate + dinitrophenyl[side 2]
substrate for MRP1
-
-
?
ATP + H2O + dipyridamole/in
ADP + phosphate + dipyridamole/out
-
-
-
-
?
ATP + H2O + dipyridamole[side 1]
ADP + phosphate + dipyridamole[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + docetaxel/in
ADP + phosphate + docetaxel/out
-
-
-
-
?
ATP + H2O + docetaxel[side 1]
ADP + phosphate + docetaxel[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + dodecyloctaglycol/in
ADP + phosphate + dodecyloctaglycol/out
-
-
-
-
?
ATP + H2O + doxorubicin/in
ADP + phosphate + doxorubicin/out
ATP + H2O + doxorubicin[side 1]
ADP + phosphate + doxorubicin[side 2]
ATP + H2O + doxycycline[side 1]
ADP + phosphate + doxycycline[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + E217betaG/in
ADP + phosphate + E217betaG/out
-
MRP3 preferentially transports E217betaG with a medium affinity and a very high capacity, while MRP1 transports E217betaG with a higher affinity but with much lower capacity
-
-
?
ATP + H2O + echonocandin B[side 1]
ADP + phosphate + echonocandin B[side 2]
-
-
-
-
?
ATP + H2O + edaravone glucuronide/in
ADP + phosphate + edaravone glucuronide/out
-
-
-
-
?
ATP + H2O + endosulfan[side 1]
ADP + phosphate + endosulfan[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + epirubicin[side 1]
ADP + phosphate + epirubicin[side 2]
substrate for P-glycoprotein, BCRP, and MPR2
-
-
?
ATP + H2O + epothilone B/in
ADP + phosphate + epothilone B/out
-
-
-
-
?
ATP + H2O + erythromycin[side 1]
ADP + phosphate + erythromycin[side 2]
ATP + H2O + estradiol 17-beta-D-glucuronide/in
ADP + phosphate + estradiol 17-beta-D-glucuronide/out
-
-
-
-
?
ATP + H2O + estradiol glucuronide/in
ADP + phosphate + estradiol glucuronide/out
-
-
-
-
?
ATP + H2O + estradiol[side 1]
ADP + phosphate + estradiol[side 2]
substrate for MRP1
-
-
?
ATP + H2O + estrone-3-sulfate/in
ADP + phosphate + estrone-3-sulfate/out
ATP + H2O + estrone-3-sulfate[side 1]
ADP + phosphate + estrone-3-sulfate[side 2]
ATP + H2O + estrone[side 1]
ADP + phosphate + estrone[side 2]
substrate for MRP1
-
-
?
ATP + H2O + ethacrynic acid[side 1]
ADP + phosphate + ethacrynic acid[side 2]
substrate for MRP1
-
-
?
ATP + H2O + ethanol/in
ADP + phosphate + ethanol/out
ATP + H2O + ethidium bromide/in
ADP + phosphate + ethidium bromide/out
ATP + H2O + ethidium bromide[side 1]
ADP + phosphate + ethidium bromide[side 2]
ATP + H2O + ethidium[side 1]
ADP + phosphate + ethidium[side 2]
-
-
-
-
?
ATP + H2O + ethinylestradiol-3-O-glucuronide[side 1]
ADP + phosphate + ethinylestradiol-3-O-glucuronide[side 2]
substrate for MPR2
-
-
?
ATP + H2O + etoposide/in
ADP + phosphate + etoposide/out
ATP + H2O + etoposide[side 1]
ADP + phosphate + etoposide[side 2]
ATP + H2O + felodipine[side 1]
ADP + phosphate + felodipine[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + fenbuconazole/in
ADP + phosphate + fenbuconazole/out
-
-
-
-
?
ATP + H2O + fentanyl[side 1]
ADP + phosphate + fentanyl[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + fexofenadine/in
ADP + phosphate + fexofenadine/out
-
-
-
-
?
ATP + H2O + fexofenadine[side 1]
ADP + phosphate + fexofenadine[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + FK-506[side 1]
ADP + phosphate + FK-506[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + FK506[side 1]
ADP + phosphate + FK506[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + fluconazole/in
ADP + phosphate + fluconazole/out
ATP + H2O + fluoroquinolone/in
ADP + phosphate + fluoroquinolone/out
-
-
-
-
?
ATP + H2O + fluoxetine/in
ADP + phosphate + fluoxetine/out
ATP + H2O + fluvoxamine/in
ADP + phosphate + fluvoxamine/out
ATP + H2O + folic acid/in
ADP + phosphate + folic acid/out
-
-
-
-
?
ATP + H2O + folic acid[side 1]
ADP + phosphate + folic acid[side 2]
substrate for MRP1
-
-
?
ATP + H2O + furosemide/in
ADP + phosphate + furosemide/out
ATP + H2O + gefitinib[side 1]
ADP + phosphate + gefitinib[side 2]
ATP + H2O + gemcitabine/in
ADP + phosphate + gemcitabine/out
-
-
-
-
?
ATP + H2O + genistein-7-glucoside[side 1]
ADP + phosphate + genistein-7-glucoside[side 2]
substrate for MPR2
-
-
?
ATP + H2O + genistein[side 1]
ADP + phosphate + genistein[side 2]
ATP + H2O + gentamicin[side 1]
ADP + phosphate + gentamicin[side 2]
-
-
-
-
?
ATP + H2O + glaucine/in
ADP + phosphate + glaucine/out
-
-
-
-
?
ATP + H2O + glutathione disulfide[side 1]
ADP + phosphate + glutathione disulfide[side 2]
substrate for MRP1
-
-
?
ATP + H2O + glutathione/in
ADP + phosphate + glutathione/out
-
-
-
-
?
ATP + H2O + glycocholic acid[side 1]
ADP + phosphate + glycocholic acid[side 2]
-
-
-
?
ATP + H2O + gramicidin A[side 1]
ADP + phosphate + gramicidin A[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + gramicidin D[side 1]
ADP + phosphate + gramicidin D[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + grepafloxacine[side 1]
ADP + phosphate + grepafloxacine[side 2]
substrate for MPR2
-
-
?
ATP + H2O + grepafloxacin[side 1]
ADP + phosphate + grepafloxacin[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + GSH-conjugated 4-hydroxy-2-nonenal/in
ADP + phosphate + GSH-conjugated 4-hydroxy-2-nonenal/out
-
-
-
-
?
ATP + H2O + GSH-conjugated prostaglandin A2/in
ADP + phosphate + GSH-conjugated prostaglandin A2/out
-
-
-
-
?
ATP + H2O + GSSG/in
ADP + phosphate + GSSG/out
-
-
-
-
?
ATP + H2O + H33342/in
ADP + phosphate + H33342/out
-
-
-
-
?
ATP + H2O + hematoporphyrin[side 1]
ADP + phosphate + hematoporphyrin[side 2]
substrate for BCRP
-
-
?
ATP + H2O + Hoechst 33342/in
ADP + phosphate + Hoechst 33342/out
ATP + H2O + Hoechst 33342[side 1]
ADP + phosphate + Hoechst 33342[side 2]
ATP + H2O + Hoechst33342[side 1]
ADP + phosphate + Hoechst33342[side 2]
ATP + H2O + hydrochlorothiazide/in
ADP + phosphate + hydrochlorothiazide/out
-
-
-
-
?
ATP + H2O + hydroxyurea[side 1]
ADP + phosphate + hydroxyurea[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + hydroxyzine/in
ADP + phosphate + hydroxyzine/out
ATP + H2O + imatinib[side 1]
ADP + phosphate + imatinib[side 2]
substrate for BCRP
-
-
?
ATP + H2O + indinavir[side 1]
ADP + phosphate + indinavir[side 2]
ATP + H2O + indomethacin/in
ADP + phosphate + indomethacin/out
ATP + H2O + iodoarylazidoprazosin[side 1]
ADP + phosphate + iodoarylazidoprazosin[side 2]
ATP + H2O + irinotecan[side 1]
ADP + phosphate + irinotecan[side 2]
substrate for P-glycoprotein, BCRP, and MPR2
-
-
?
ATP + H2O + itraconazole/in
ADP + phosphate + itraconazole/out
ATP + H2O + itraconazole[side 1]
ADP + phosphate + itraconazole[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + kanamycin[side 1]
ADP + phosphate + kanamycin[side 2]
-
-
-
-
?
ATP + H2O + ketoconazole/in
ADP + phosphate + ketoconazole/out
ATP + H2O + ketoconazole[side 1]
ADP + phosphate + ketoconazole[side 2]
ATP + H2O + lamivudine[side 1]
ADP + phosphate + lamivudine[side 2]
substrate for BCRP
-
-
?
ATP + H2O + latanoprost/in
ADP + phosphate + latanoprost/out
-
-
-
-
?
ATP + H2O + leucovorin/in
ADP + phosphate + leucovorin/out
-
-
-
-
?
ATP + H2O + leucovorin[side 1]
ADP + phosphate + leucovorin[side 2]
substrate for MRP1
-
-
?
ATP + H2O + leukotriene B4/in
ADP + phosphate + leukotriene B4/out
-
MRP4 only transports leukotriene B4 in the presence of glutathione
-
-
?
ATP + H2O + leukotriene C4/in
ADP + phosphate + leukotriene C4/out
ATP + H2O + leukotriene C4[side 1]
ADP + phosphate + leukotriene C4[side 2]
substrate for MRP1
-
-
?
ATP + H2O + leukotriene D4[side 1]
ADP + phosphate + leukotriene D4[side 2]
substrate for MRP1
-
-
?
ATP + H2O + leukotriene E4/in
ADP + phosphate + leukotriene E4/out
-
-
-
-
?
ATP + H2O + leupeptin[side 1]
ADP + phosphate + leupeptin[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + levofloxacin[side 1]
ADP + phosphate + levofloxacin[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + lidocaine[side 1]
ADP + phosphate + lidocaine[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + Lipid A/in
ADP + phosphate + Lipid A/out
-
native LmrA
-
-
?
ATP + H2O + lithocholic acid[side 1]
ADP + phosphate + lithocholic acid[side 2]
-
-
-
?
ATP + H2O + loperamide/in
ADP + phosphate + loperamide/out
ATP + H2O + lopinavir[side 1]
ADP + phosphate + lopinavir[side 2]
ATP + H2O + loratadine/in
ADP + phosphate + loratadine/out
-
-
-
-
?
ATP + H2O + lovastatin[side 1]
ADP + phosphate + lovastatin[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + lyso-tracker green[side 1]
ADP + phosphate + lyso-tracker green[side 2]
-
-
-
?
ATP + H2O + lysophosphatidylinositol/in
ADP + phosphate + lysophosphatidylinositol/out
-
-
-
-
?
ATP + H2O + malachite green/in
ADP + phosphate + malachite green/out
-
-
-
-
?
ATP + H2O + melphalan[side 1]
ADP + phosphate + melphalan[side 2]
substrate for MRP1
-
-
?
ATP + H2O + methotrexate/in
ADP + phosphate + methotrexate/out
ATP + H2O + methotrexate[side 1]
ADP + phosphate + methotrexate[side 2]
ATP + H2O + methyl parathion[side 1]
ADP + phosphate + methyl parathion[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + miconazole/in
ADP + phosphate + miconazole/out
ATP + H2O + miconazolenitrate[side 1]
ADP + phosphate + miconazolenitrate[side 2]
ATP + H2O + midazolam/in
ADP + phosphate + midazolam/out
ATP + H2O + minocycline[side 1]
ADP + phosphate + minocycline[side 2]
-
-
-
-
?
ATP + H2O + misoprostol/in
ADP + phosphate + misoprostol/out
-
-
-
-
?
ATP + H2O + mitomycin C[side 1]
ADP + phosphate + mitomycin C[side 2]
ATP + H2O + mitoxantrone/in
ADP + phosphate + mitoxantrone/out
-
-
-
-
?
ATP + H2O + mitoxantrone[side 1]
ADP + phosphate + mitoxantrone[side 2]
ATP + H2O + monensin/in
ADP + phosphate + monensin/out
-
affinity of verapamil to MDR1 is not affected by pH value. Protein concentration is inversely related to the maximum activation of ATPase activity achieved
-
-
?
ATP + H2O + monoglucuronosyl bilirubin/in
ADP + phosphate + monoglucuronosyl bilirubin/out
-
-
-
-
?
ATP + H2O + morphine[side 1]
ADP + phosphate + morphine[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + MTS-rhodamine [side 1]
ADP + phosphate + MTS-rhodamine [side 2]
the binding site in transmembrane segment 5 is F343C for rhodamine
-
-
?
ATP + H2O + N-(1-phenylcyclohexyl)-3-ethoxypropanamine/in
ADP + phosphate + N-(1-phenylcyclohexyl)-3-ethoxypropanamine/out
-
-
-
-
?
ATP + H2O + N-(2'-deoxy-beta-D-ribofuranosyl)-5-cyclohexyl-1H-indole/in
?
-
nontransported substrate of P-glycoprotein
-
-
?
ATP + H2O + N-benzyl-2-nitro-1H-imidazole-1-acetamide/in
ADP + phosphate + N-benzyl-2-nitro-1H-imidazole-1-acetamide/out
ATP + H2O + N-ethylmaleimide S-glutathione/in
ADP + phosphate + N-ethylmaleimide S-glutathione/out
ATP + H2O + N-isopropyl-1,2-diphenylethylamine/in
ADP + phosphate + N-isopropyl-1,2-diphenylethylamine/out
-
-
-
-
?
ATP + H2O + nelfinavir[side 1]
ADP + phosphate + nelfinavir[side 2]
ATP + H2O + nicardipine/in
ADP + phosphate + nicardipine/out
-
-
-
-
?
ATP + H2O + nicardipine[side 1]
ADP + phosphate + nicardipine[side 2]
substrate for BCRP
-
-
?
ATP + H2O + nifedipine/in
ADP + phosphate + nifedipine/out
-
-
-
-
?
ATP + H2O + nifedipine[side 1]
ADP + phosphate + nifedipine[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + nisoldipine[side 1]
ADP + phosphate + nisoldipine[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + nitrendipine[side 1]
ADP + phosphate + nitrendipine[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + norfloxacin[side 1]
ADP + phosphate + norfloxacin[side 2]
ATP + H2O + nortryptiline/in
ADP + phosphate + nortryptiline/out
ATP + H2O + ochratoxin A[side 1]
ADP + phosphate + ochratoxin A[side 2]
ATP + H2O + ofloxacin[side 1]
ADP + phosphate + ofloxacin[side 2]
ATP + H2O + oligomycin/in
ADP + phosphate + oligomycin/out
-
-
-
-
?
ATP + H2O + olmesartan/in
ADP + phosphate + olmesartan/out
-
-
-
-
?
ATP + H2O + olmesartan[side 1]
ADP + phosphate + olmesartan[side 2]
substrate for MPR2
-
-
?
ATP + H2O + ortataxel[side 1]
ADP + phosphate + ortataxel[side 2]
substrate for BCRP
-
-
?
ATP + H2O + p-methoxy-ethylamphetamine/in
ADP + phosphate + p-methoxy-ethylamphetamine/out
ATP + H2O + paclitaxel/in
ADP + phosphate + paclitaxel/out
ATP + H2O + para-methoxy-ethylamphetamine/in
ADP + phosphate + para-methoxy-ethylamphetamine/out
-
-
-
-
?
ATP + H2O + paraquat[side 1]
ADP + phosphate + paraquat[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + paroxetine/in
ADP + phosphate + paroxetine/out
ATP + H2O + pentazocine[side 1]
ADP + phosphate + pentazocine[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + pepstatin A[side 1]
ADP + phosphate + pepstatin A[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + phenothiazine[side 1]
ADP + phosphate + phenothiazine[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + pheophorbide A[side 1]
ADP + phosphate + pheophorbide A[side 2]
-
-
-
?
ATP + H2O + phloridzin[side 1]
ADP + phosphate + phloridzin[side 2]
substrate for MPR2
-
-
?
ATP + H2O + phosphatidylcholine/in
ADP + phosphate + phosphatidylcholine/out
-
-
-
?
ATP + H2O + pirarubicin/in
ADP + phosphate + pirarubicin/out
-
-
-
-
?
ATP + H2O + pravastatin[side 1]
ADP + phosphate + pravastatin[side 2]
substrate for BCRP
-
-
?
ATP + H2O + prazosin/in
ADP + phosphate + prazosin/out
ATP + H2O + prazosin[side 1]
ADP + phosphate + prazosin[side 2]
-
-
-
?
ATP + H2O + prednisone/in
ADP + phosphate + prednisone/out
ATP + H2O + probenecid/in
ADP + phosphate + probenecid/out
ATP + H2O + progesterone/in
ADP + phosphate + progesterone/out
ATP + H2O + progesterone[side 1]
ADP + phosphate + progesterone[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + propafenone[side 1]
ADP + phosphate + propafenone[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + propoxyphene/in
ADP + phosphate + propoxyphene/out
ATP + H2O + prostaglandin A2/in
ADP + phosphate + prostaglandin A2/out
-
-
-
-
?
ATP + H2O + prostaglandin E1/in
ADP + phosphate + prostaglandin E1/out
-
-
-
-
?
ATP + H2O + prostaglandin E2/in
ADP + phosphate + prostaglandin E2/out
-
-
-
-
?
ATP + H2O + prostaglandin E2[side 1]
ADP + phosphate + prostaglandin E2[side 2]
substrate for MRP1
-
-
?
ATP + H2O + prostaglandin F2alpha/in
ADP + phosphate + prostaglandin F2alpha/out
-
-
-
-
?
ATP + H2O + PSC-833[side 1]
ADP + phosphate + PSC-833[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + puromycin/in
ADP + phosphate + puromycin/out
-
-
-
-
?
ATP + H2O + quercetin 4'-beta-glucoside[side 1]
ADP + phosphate + quercetin 4'-beta-glucoside[side 2]
substrate for MPR2
-
-
?
ATP + H2O + quercetin[side 1]
ADP + phosphate + quercetin[side 2]
ATP + H2O + quinidine/in
ADP + phosphate + quinidine/out
ATP + H2O + quinidine[side 1]
ADP + phosphate + quinidine[side 2]
ATP + H2O + ranitidine[side 1]
ADP + phosphate + ranitidine[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + rapamycin[side 1]
ADP + phosphate + rapamycin[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + repaglinide/in
ADP + phosphate + repaglinide/out
-
-
-
-
?
ATP + H2O + resazurine/in
ADP + phosphate + resazurine/out
-
-
-
-
?
ATP + H2O + reserpine[side 1]
ADP + phosphate + reserpine[side 2]
substrate for BCRP
-
-
?
ATP + H2O + resorufine/in
ADP + phosphate + resorufine/out
-
-
-
-
?
ATP + H2O + resveratrol disulfate/in
ADP + phosphate + resveratrol disulfate/out
-
substrate of BCRP in vitro
-
-
?
ATP + H2O + resveratrol-3-glucuronide/in
ADP + phosphate + resveratrol-3-glucuronide/out
-
substrate of Mrp3 and BCRP in vitro as sulfate
-
-
?
ATP + H2O + resveratrol-3-sulfate [side 1]
ADP + phosphate + resveratrol-3-sulfate [side 2]
-
-
-
-
?
ATP + H2O + resveratrol/in
ADP + phosphate + resveratrol/out
-
substrate of BCRP in vitro as sulfate
-
-
?
ATP + H2O + rhodamine 123 /in
ADP + phosphate + rhodamine 123 /out
-
-
-
-
?
ATP + H2O + rhodamine 123/in
ADP + phosphate + rhodamine 123/out
ATP + H2O + rhodamine 123[side 1]
ADP + phosphate + rhodamine 123[side 2]
ATP + H2O + rhodamine 6-G/in
ADP + phosphate + rhodamine 6-G/out
-
-
-
-
?
ATP + H2O + rhodamine 6G/in
ADP + phosphate + rhodamine 6G/out
ATP + H2O + rhodamine 6G[side 1]
ADP + phosphate + rhodamine 6G[side 2]
ATP + H2O + rhodamine B/in
ADP + phosphate + rhodamine B/out
-
-
-
-
?
ATP + H2O + rhodamine B[side 1]
ADP + phosphate + rhodamine B[side 2]
-
-
-
-
?
ATP + H2O + rhodamine-123[side 1]
ADP + phosphate + rhodamine-123[side 2]
-
-
-
-
?
ATP + H2O + riboflavin[side 1]
ADP + phosphate + riboflavin[side 2]
ATP + H2O + rifampicin/in
ADP + phosphate + rifampicin/out
-
-
-
?
ATP + H2O + rifampicin[side 1]
ADP + phosphate + rifampicin[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + rifampin[side 1]
ADP + phosphate + rifampin[side 2]
-
-
-
-
?
ATP + H2O + risperidone/in
ADP + phosphate + risperidone/out
ATP + H2O + ritonavir/in
ADP + phosphate + ritonavir/out
ATP + H2O + ritonavir[side 1]
ADP + phosphate + ritonavir[side 2]
ATP + H2O + rosuvastatin[side 1]
ADP + phosphate + rosuvastatin[side 2]
substrate for BCRP
-
-
?
ATP + H2O + S-2,4-dinitrophenylglutathione/in
ADP + phosphate + S-2,4-dinitrophenylglutathione/out
ATP + H2O + salmeterol/in
ADP + phosphate + salmeterol/out
-
-
-
-
?
ATP + H2O + saquinavir/in
ADP + phosphate + saquinavir/out
-
-
-
-
?
ATP + H2O + saquinavir[side 1]
ADP + phosphate + saquinavir[side 2]
ATP + H2O + sertraline/in
ADP + phosphate + sertraline/out
ATP + H2O + simvastatin[side 1]
ADP + phosphate + simvastatin[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + sirolimus[side 1]
ADP + phosphate + sirolimus[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + SN-38/in
ADP + phosphate + SN-38/out
-
-
-
-
?
ATP + H2O + SN-38[side 1]
ADP + phosphate + SN-38[side 2]
ATP + H2O + sparfloxacin[side 1]
ADP + phosphate + sparfloxacin[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + sphingosine-1-phosphate/in
ADP + phosphate + sphingosine-1-phosphate/out
-
-
-
-
?
ATP + H2O + staurosporine[side 1]
ADP + phosphate + staurosporine[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + tacrolimus[side 1]
ADP + phosphate + tacrolimus[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + talinolol/in
ADP + phosphate + talinolol/out
-
-
-
-
?
ATP + H2O + tamoxifen[side 1]
ADP + phosphate + tamoxifen[side 2]
ATP + H2O + tariquidar [side 1]
ADP + phosphate + tariquidar [side 2]
-
-
-
?
ATP + H2O + taurochenodeoxycholic acid[side 1]
ADP + phosphate + taurochenodeoxycholic acid[side 2]
-
-
-
?
ATP + H2O + taurocholate/in
ADP + phosphate + taurocholate/out
-
-
-
-
?
ATP + H2O + taurocholic acid[side 1]
ADP + phosphate + taurocholic acid[side 2]
-
-
-
?
ATP + H2O + taurodeoxycholic acid[side 1]
ADP + phosphate + taurodeoxycholic acid[side 2]
-
-
-
?
ATP + H2O + taurolithocholic acid[side 1]
ADP + phosphate + taurolithocholic acid[side 2]
-
-
-
?
ATP + H2O + taxol[side 1]
ADP + phosphate + taxol[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + telmisartan/in
ADP + phosphate + telmisartan/out
-
-
-
-
?
ATP + H2O + temocaprilate[side 1]
ADP + phosphate + temocaprilate[side 2]
substrate for MPR2
-
-
?
ATP + H2O + temozolomide[side 1]
ADP + phosphate + temozolomide[side 2]
substrate for ABCB1
-
-
?
ATP + H2O + teniposide[side 1]
ADP + phosphate + teniposide[side 2]
ATP + H2O + tenofovir/in
ADP + phosphate + tenofovir/out
-
-
-
-
?
ATP + H2O + terfenadine[side 1]
ADP + phosphate + terfenadine[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + tetracycline[side 1]
ADP + phosphate + tetracycline[side 2]
ATP + H2O + tetramethylrhodamine/in
ADP + phosphate + tetramethylrhodamine/out
-
better substrate than rhodamine 123, temperature dependence of the rate of tetramethylrosamine transport, the rate of drug transport may be dominated by partitioning of drug into the membrane bilayer
-
-
?
ATP + H2O + tetramethylrosamine/in
ADP + phosphate + tetramethylrosamine/out
ATP + H2O + thromboxane B2/in
ADP + phosphate + thromboxane B2/out
-
-
-
-
?
ATP + H2O + tiapamil[side 1]
ADP + phosphate + tiapamil[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + topotecan/in
ADP + phosphate + topotecan/out
-
-
-
-
?
ATP + H2O + topotecan[side 1]
ADP + phosphate + topotecan[side 2]
ATP + H2O + trans-flupentixol[side 1]
ADP + phosphate + trans-flupentixol[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + trans-resveratrol[side 1]
ADP + phosphate + trans-resveratrol[side 2]
ATP + H2O + trazodone/in
ADP + phosphate + trazodone/out
ATP + H2O + trifluoperazine[side 1]
ADP + phosphate + trifluoperazine[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + Triton X-100/in
ADP + phosphate + Triton X-100/out
ATP + H2O + Tween 80/in
ADP + phosphate + Tween 80/out
ATP + H2O + urate/in
ADP + phosphate + urate/out
ATP + H2O + ursodeoxycholylglycine/in
ADP + phosphate + ursodeoxycholylglycine/out
-
-
-
-
?
ATP + H2O + ursodeoxycholyltaurine/in
ADP + phosphate + ursodeoxycholyltaurine/out
-
-
-
-
?
ATP + H2O + valinomycin/in
ADP + phosphate + valinomycin/out
ATP + H2O + valinomycin[side 1]
ADP + phosphate + valinomycin[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + valspodar[side 1]
ADP + phosphate + valspodar[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + verapamil [side 1]
ADP + phosphate + verapamil [side 2]
the binding site in transmembrane segment 5 is I306C for verapamil
-
-
?
ATP + H2O + verapamil/in
ADP + phosphate + verapamil/out
ATP + H2O + verapamil[side 1]
ADP + phosphate + verapamil[side 2]
ATP + H2O + vinblastine sulfate/in
ADP + phosphate + vinblastine sulfate/out
-
-
-
?
ATP + H2O + vinblastine/in
ADP + phosphate + vinblastine/out
ATP + H2O + vinblastine[side 1]
ADP + phosphate + vinblastine[side 2]
ATP + H2O + vincristine sulfate/in
ADP + phosphate + vincristine sulfate/out
-
-
-
?
ATP + H2O + vincristine/in
ADP + phosphate + vincristine/out
-
-
-
-
?
ATP + H2O + vincristine[side 1]
ADP + phosphate + vincristine[side 2]
ATP + H2O + VP-16/in
ADP + phosphate + VP-16/out
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
ATP + H2O + xenobiotic[side 1]
ADP + phosphate + xenobiotic[side 2]
ATP + H2O + zidovudine[side 1]
ADP + phosphate + zidovudine[side 2]
substrate for BCRP
-
-
?
ATP + H2O + zolpidem/in
ADP + phosphate + zolpidem/out
ATP + H2O + [1,2,6,7-3H(N)]dehydroepiandrosterone-3-sulfate/in
ADP + phosphate + [1,2,6,7-3H(N)]dehydroepiandrosterone-3-sulfate/out
-
-
-
-
?
bacitracin/in + ATP + H2O
bacitracin/out + ADP + phosphate
-
-
-
?
chloramphenicol/in + ATP + H2O
chloramphenicol/out + ADP + phosphate
-
-
-
?
clotrimazole/in + ATP + H2O
clotrimazole/out + ADP + phosphate
-
-
-
-
?
colchicine/in + ATP + H2O
colchicine/out + ADP + phosphate
-
-
-
?
CTP + H2O
CDP + phosphate
-
-
-
-
?
CTP + H2O + rhodamine 6G/in
CDP + phosphate + rhodamine 6G/out
-
low CTPase activity
-
-
?
cyclo(D-Trp-D-Asp-L-Pro-D-Val-L-Leu)/in + ATP + H2O
cyclo(D-Trp-D-Asp-L-Pro-D-Val-L-Leu)/out + ADP + phosphate
cysteinyl leukotriene C4/in + ATP + H2O
cysteinyl leukotriene C4/out + ADP + phosphate
-
-
-
?
daunomycin/in + ATP + H2O
daunomycin/out + ADP + phosphate
-
-
-
?
daunorubicin/in + ATP + H2O
daunorubicin/out + ADP + phosphate
dexamethasone/in + ATP + H2O
dexamethasone/out + ADP + phosphate
-
-
-
-
?
digoxin/in + ATP + H2O
digoxin/out + ADP + phosphate
-
-
-
-
?
doxorubicin/in + ATP + H2O
doxorubicin/out + ADP + phosphate
epsilon-ATP + H2O
? + phosphate
-
-
-
-
?
erythromycin/in + ATP + H2O
erythromycin/out + ADP + phosphate
estradiol 17-beta-D-glucuronide/in + ATP + H2O
estradiol 17-beta-D-glucuronide/out + ADP + phosphate
ethidium bromide/in + ATP + H2O
ethidium bromide/out + ADP + phosphate
-
-
-
?
etoposide/in + ATP + H2O
etoposide/out + ADP + phosphate
glycocholate/in + ATP + H2O
glycocholate/out + ADP + phosphate
-
-
-
?
GSH/in + ATP + H2O
GSH/out + ADP + phosphate
-
-
-
?
GTP + H2O
GDP + phosphate
GTP + H2O + ciprofloxacin[side 1]
GDP + phosphate + ciprofloxacin[side 2]
-
the enzyme has much higher GTPase activity as compared to its ATPase activity
-
-
?
GTP + H2O + doxorubicin/in
GDP + phosphate + doxorubicin/out
highest efficiency
-
-
?
GTP + H2O + doxorubicin[side 1]
GDP + phosphate + doxorubicin[side 2]
-
the enzyme has much higher GTPase activity as compared to its ATPase activity
-
-
?
GTP + H2O + Hoechst33342[side 1]
GDP + phosphate + Hoechst33342[side 2]
-
the enzyme has much higher GTPase activity as compared to its ATPase activity. Hoechst 33342 is 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole
-
-
?
GTP + H2O + norfloxacin[side 1]
GDP + phosphate + norfloxacin[side 2]
-
the enzyme has much higher GTPase activity as compared to its ATPase activity
-
-
?
GTP + H2O + rhodamine 6G/in
GDP + phosphate + rhodamine 6G/out
-
-
-
-
?
Hoechst 33342/in + ATP + H2O
Hoechst 33342/out + ADP + H2O
-
i.e. 2-[2-(4-ethoxyphenyl)-6-benzimidazolyl]-6-(1-methyl-4-piperazinyl)benzimidazole
-
?
leukotriene C4/in + ATP + H2O
leukotriene C4/out + ADP + phosphate
leukotriene D4/in + ATP + H2O
leukotriene D4/out + ADP + phosphate
leukotriene E4/in + ATP + H2O
leukotriene E4/out + ADP + phosphate
-
-
-
?
methotrexate/in + ATP + H2O
methotrexate/out + ADP + phosphate
-
-
-
?
N-methyl-N-(9-phenyl-2,3,6,7-tetrahydro-1H,5H,12H-pyrido[3,2,1-ij]selenochromeno[2,3-f]quinolin-12-ylidene)methanaminium hexafluorophosphate/in + ATP + H2O
N-methyl-N-(9-phenyl-2,3,6,7-tetrahydro-1H,5H,12H-pyrido[3,2,1-ij]thiochromeno[2,3-f]quinolin-12-ylidene)methanaminium hexafluorophosphate/out + ADP + phosphate
-
-
-
-
?
nicardipine/in + ATP + H2O
nicardipine/out + ADP + phosphate
-
-
-
-
?
novobiocin/in + ATP + H2O
novobiocin/out + ADP + phosphate
-
-
-
?
oleandomycin/in + ATP + H2O
oleandomycin/out + ADP + phosphate
paclitaxel/in + ATP + H2O
paclitaxel/out + ADP + phosphate
-
-
-
-
?
pentachlorophenol/in + ATP + H2O
pentachlorophenol/out + ADP + phosphate
-
-
-
?
phenol/in + ATP + H2O
phenol/out + ADP + phosphate
-
-
-
?
rhodamine 123/in + ATP + H2O
rhodamine 123/out + ADP + phosphate
rhodamine B/in + ATP + H2O
rhodamine B/out + ADP + phosphate
-
-
-
-
?
S-(2,4-dinitrophenyl)glutathione/in + ATP + H2O
S-(2,4-dinitrophenyl)glutathione/out + ADP + phosphate
spiramycin/in + ATP + H2O
spiramycin/out + ADP + phosphate
streptomycin/in + ATP + H2O
streptomycin/out + ADP + phosphate
-
-
-
?
streptothricin/in + ATP + H2O
streptothricin/out + ADP + phosphate
-
-
-
?
taxol/in + ATP + H2O
taxol/out + ADP + H2O
-
weak activity
-
?
tetrachlorohydroquinone/in + ATP + H2O
tetrachlorohydroquinone/out + ADP + phosphate
-
-
-
?
tetracyclin/in + ATP + H2O
tetracyclin/out + ADP + phosphate
tobramycin/in + ATP + H2O
tobramycin/out + ADP + phosphate
-
-
-
?
UTP + H2O
UDP + phosphate
UTP + H2O + rhodamine 6G/in
UDP + phosphate + rhodamine 6G/out
-
low UTPase activity
-
-
?
valinomycin/in + ATP + H2O
valinomycin/out + ADP + phosphate
-
-
-
-
?
verapamil/in + ATP + H2O
verapamil/out + ADP + phosphate
-
-
-
-
?
vinblastine/in + ATP + H2O
vinblastine/out + ADP + phosphate
vincristine/in + ATP + H2O
vincristine/out + ADP + phosphate
additional information
?
-
aflatoxin B1/in + ATP + H2O
aflatoxin B1/out + ADP + phosphate
-
-
-
?
aflatoxin B1/in + ATP + H2O
aflatoxin B1/out + ADP + phosphate
-
-
-
?
ATP + H2O
ADP + phosphate
-
ATP binding to Cdr1p is not a prerequisite for drug binding and both drug as well as ATP binding, which induce specific conformational changes, can occur independently of each other
-
-
?
ATP + H2O
ADP + phosphate
-
-
-
-
?
ATP + H2O
ADP + phosphate
-
-
-
-
?
ATP + H2O
ADP + phosphate
-
-
-
-
?
ATP + H2O
ADP + phosphate
-
-
-
-
?
ATP + H2O
ADP + phosphate
-
-
-
-
?
ATP + H2O + 17beta-estradiol 17-(beta-D-glucuronide)/in
ADP + phosphate + 17beta-estradiol 17-(beta-D-glucuronide)/out
-
-
-
-
?
ATP + H2O + 17beta-estradiol 17-(beta-D-glucuronide)/in
ADP + phosphate + 17beta-estradiol 17-(beta-D-glucuronide)/out
-
transported by MRP1 and MRP3
-
-
?
ATP + H2O + 17beta-estradiol 17-(beta-D-glucuronide)/in
ADP + phosphate + 17beta-estradiol 17-(beta-D-glucuronide)/out
-
-
-
-
?
ATP + H2O + 2',7'-bis-(2-carboxyethyl)-5,6-carboxylfluoresceinacetoxymethyl ester/in
ADP + phosphate + 2',7'-bis-(2-carboxyethyl)-5,6-carboxylfluoresceinacetoxymethyl ester/out
YdaG/YdbA heterodimer
-
-
?
ATP + H2O + 2',7'-bis-(2-carboxyethyl)-5,6-carboxylfluoresceinacetoxymethyl ester/in
ADP + phosphate + 2',7'-bis-(2-carboxyethyl)-5,6-carboxylfluoresceinacetoxymethyl ester/out
YdaG/YdbA heterodimer
-
-
?
ATP + H2O + 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole/in
ADP + phosphate + 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole/out
-
Hoechst 33342
-
-
?
ATP + H2O + 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole/in
ADP + phosphate + 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole/out
-
Hoechst 33342, ABC transporter YvcC
-
-
?
ATP + H2O + 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole/in
ADP + phosphate + 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole/out
-
Hoechst 33342, half-ABC transporter BmrA, Glu-504, adjacent to the Walker-B motif, is the catalytic base for ATP hydrolysis
-
-
?
ATP + H2O + 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole/in
ADP + phosphate + 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole/out
-
Hoechst 33342 binding site, proximity of bound Hoechst 33342 to the ATPase catalytic sites places the drug binding site of P-glycoprotein within the cytoplasmic membrane leaflet, Cys-428 and Cys-1071 are within the catalytic sites of Pgp, one within each of the Walker A motifs of the nucleotide binding folds, mechanism
-
-
?
ATP + H2O + 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole/in
ADP + phosphate + 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole/out
-
Hoechst 33342
-
-
?
ATP + H2O + 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole/in
ADP + phosphate + 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole/out
-
Hoechst 33342
-
-
?
ATP + H2O + 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole/in
ADP + phosphate + 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole/out
Hoechst 33342, YdaG/YdbA heterodimer
-
-
?
ATP + H2O + 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole/in
ADP + phosphate + 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole/out
Hoechst 33342, YdaG/YdbA heterodimer
-
-
?
ATP + H2O + 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole/in
ADP + phosphate + 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole/out
-
Hoechst 33342
-
-
?
ATP + H2O + 2,3,5-triphenylterazolium chloride[side 1]
ADP + phosphate + 2,3,5-triphenylterazolium chloride[side 2]
-
-
-
-
?
ATP + H2O + 2,3,5-triphenylterazolium chloride[side 1]
ADP + phosphate + 2,3,5-triphenylterazolium chloride[side 2]
-
-
-
-
?
ATP + H2O + 2,4-dinitrophenyl-S-glutathione[side 1]
ADP + phosphate + 2,4-dinitrophenyl-S-glutathione[side 2]
-
-
-
?
ATP + H2O + 2,4-dinitrophenyl-S-glutathione[side 1]
ADP + phosphate + 2,4-dinitrophenyl-S-glutathione[side 2]
-
-
-
?
ATP + H2O + 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine[side 1]
ADP + phosphate + 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine[side 2]
-
-
-
?
ATP + H2O + 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine[side 1]
ADP + phosphate + 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine[side 2]
-
-
-
?
ATP + H2O + 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine[side 1]
ADP + phosphate + 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine[side 2]
-
-
-
?
ATP + H2O + 3,3'-dihexyloxacarbocyanine iodide/in
ADP + phosphate + 3,3'-dihexyloxacarbocyanine iodide/out
-
-
-
-
?
ATP + H2O + 3,3'-dihexyloxacarbocyanine iodide/in
ADP + phosphate + 3,3'-dihexyloxacarbocyanine iodide/out
-
-
-
-
?
ATP + H2O + 4-N-(2'-methoxystyryl)-thiosemicarbazone/in
ADP + phosphate + 4-N-(2'-methoxystyryl)-thiosemicarbazone/out
-
-
-
-
?
ATP + H2O + 4-N-(2'-methoxystyryl)-thiosemicarbazone/in
ADP + phosphate + 4-N-(2'-methoxystyryl)-thiosemicarbazone/out
-
-
-
-
?
ATP + H2O + 5-fluorouracil[side 1]
ADP + phosphate + 5-fluorouracil[side 2]
substrate for ABCB1
-
-
?
ATP + H2O + 5-fluorouracil[side 1]
ADP + phosphate + 5-fluorouracil[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + 9-hydroxyrisperidone/in
ADP + phosphate + 9-hydroxyrisperidone/out
-
-
-
-
?
ATP + H2O + 9-hydroxyrisperidone/in
ADP + phosphate + 9-hydroxyrisperidone/out
-
-
-
-
?
ATP + H2O + acriflavine [side 1]
ADP + phosphate + acriflavine[side 2]
-
-
-
-
?
ATP + H2O + acriflavine [side 1]
ADP + phosphate + acriflavine[side 2]
-
-
-
-
?
ATP + H2O + actinomycin D[side 1]
ADP + phosphate + actinomycin D[side 2]
-
-
-
?
ATP + H2O + actinomycin D[side 1]
ADP + phosphate + actinomycin D[side 2]
-
-
-
?
ATP + H2O + actinomycin D[side 1]
ADP + phosphate + actinomycin D[side 2]
substrate for ABCB1
-
-
?
ATP + H2O + actinomycin D[side 1]
ADP + phosphate + actinomycin D[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + amiodarone[side 1]
ADP + phosphate + amiodarone[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + amiodarone[side 1]
ADP + phosphate + amiodarone[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + anisomycin/in
ADP + phosphate + anisomycin/out
-
-
-
-
?
ATP + H2O + anisomycin/in
ADP + phosphate + anisomycin/out
-
recombinant Cdr1p
-
-
?
ATP + H2O + azidopine[side 1]
ADP + phosphate + azidopine[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + azidopine[side 1]
ADP + phosphate + azidopine[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + buspirone/in
ADP + phosphate + buspirone/out
-
-
-
-
?
ATP + H2O + buspirone/in
ADP + phosphate + buspirone/out
-
-
-
-
?
ATP + H2O + calcein/in
ADP + phosphate + calcein/out
-
-
-
-
?
ATP + H2O + calcein/in
ADP + phosphate + calcein/out
-
-
-
-
?
ATP + H2O + calcein/in
ADP + phosphate + calcein/out
-
fluorescent substrate of MRP1
-
-
?
ATP + H2O + calcein[side 1]
ADP + phosphate + calcein[side 2]
-
-
-
-
?
ATP + H2O + calcein[side 1]
ADP + phosphate + calcein[side 2]
substrate for MRP1
-
-
?
ATP + H2O + calcein[side 1]
ADP + phosphate + calcein[side 2]
-
-
-
?
ATP + H2O + ceftriaxone[side 1]
ADP + phosphate + ceftriaxone[side 2]
substrate for MPR2
-
-
?
ATP + H2O + ceftriaxone[side 1]
ADP + phosphate + ceftriaxone[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + chlorpromazine/in
ADP + phosphate + chlorpromazine/out
-
-
-
-
?
ATP + H2O + chlorpromazine/in
ADP + phosphate + chlorpromazine/out
-
-
-
-
?
ATP + H2O + cholesterol/in
ADP + phosphate + cholesterol/out
-
P-gp may actively mediate cholesterol redistribution in the cell membrane, P-gp mediates the ATP-dependent relocation of cholesterol from the cytosolic leaflet to the exoplasmic leaflet of the plasma membrane, P-gp likely contributes in stabilizing the cholesterol-rich microdomains, rafts and caveolae, and is involved in the regulation of cholesterol trafficking in cells
-
-
?
ATP + H2O + cholesterol/in
ADP + phosphate + cholesterol/out
-
P-gp may actively mediate cholesterol redistribution in the cell membrane, in the absence of substrates P-gp exhibits an apparently futile, basal ATPase activity, which is tightly dependent on the presence of cholesterol in the membrane by using native membrane vesicles containing high amounts of P-gp
-
-
?
ATP + H2O + cimetidine[side 1]
ADP + phosphate + cimetidine[side 2]
-
-
-
?
ATP + H2O + cimetidine[side 1]
ADP + phosphate + cimetidine[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + ciprofloxacin[side 1]
ADP + phosphate + ciprofloxacin[side 2]
-
-
-
-
?
ATP + H2O + ciprofloxacin[side 1]
ADP + phosphate + ciprofloxacin[side 2]
-
-
-
-
?
ATP + H2O + ciprofloxacin[side 1]
ADP + phosphate + ciprofloxacin[side 2]
substrate for BCRP
-
-
?
ATP + H2O + ciprofloxacin[side 1]
ADP + phosphate + ciprofloxacin[side 2]
-
-
-
-
?
ATP + H2O + citalopram/in
ADP + phosphate + citalopram/out
-
-
-
-
?
ATP + H2O + citalopram/in
ADP + phosphate + citalopram/out
-
-
-
-
?
ATP + H2O + clotrimazole/in
ADP + phosphate + clotrimazole/out
-
-
-
-
?
ATP + H2O + clotrimazole/in
ADP + phosphate + clotrimazole/out
-
substrate for Pdr5p
-
-
?
ATP + H2O + colchicine/in
ADP + phosphate + colchicine/out
-
-
-
-
?
ATP + H2O + colchicine/in
ADP + phosphate + colchicine/out
-
-
-
-
?
ATP + H2O + colchicine[side 1]
ADP + phosphate + colchicine[side 2]
-
-
-
?
ATP + H2O + colchicine[side 1]
ADP + phosphate + colchicine[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + colchicine[side 1]
ADP + phosphate + colchicine[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + cyclobenzaprine/in
ADP + phosphate + cyclobenzaprine/out
-
-
-
-
?
ATP + H2O + cyclobenzaprine/in
ADP + phosphate + cyclobenzaprine/out
-
-
-
-
?
ATP + H2O + cycloheximide/in
ADP + phosphate + cycloheximide/out
-
-
-
-
?
ATP + H2O + cycloheximide/in
ADP + phosphate + cycloheximide/out
-
recombinant Cdr1p
-
-
?
ATP + H2O + cycloheximide/in
ADP + phosphate + cycloheximide/out
-
-
-
-
?
ATP + H2O + cycloheximide[side 1]
ADP + phosphate + cycloheximide[side 2]
-
-
-
-
?
ATP + H2O + cycloheximide[side 1]
ADP + phosphate + cycloheximide[side 2]
-
-
-
-
?
ATP + H2O + cyclosporin A/in
ADP + phosphate + cyclosporin A/out
-
-
-
-
?
ATP + H2O + cyclosporin A/in
ADP + phosphate + cyclosporin A/out
-
-
-
-
?
ATP + H2O + cyclosporin A/in
ADP + phosphate + cyclosporin A/out
-
-
-
-
?
ATP + H2O + cyclosporin A/in
ADP + phosphate + cyclosporin A/out
-
-
-
-
?
ATP + H2O + cyclosporine A[side 1]
ADP + phosphate + cyclosporine A[side 2]
-
-
-
?
ATP + H2O + cyclosporine A[side 1]
ADP + phosphate + cyclosporine A[side 2]
-
-
-
?
ATP + H2O + cytarabine[side 1]
ADP + phosphate + cytarabine[side 2]
-
-
-
?
ATP + H2O + cytarabine[side 1]
ADP + phosphate + cytarabine[side 2]
substrate for ABCC10
-
-
?
ATP + H2O + cytarabine[side 1]
ADP + phosphate + cytarabine[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + daunomycin/in
ADP + phosphate + daunomycin/out
-
-
-
-
?
ATP + H2O + daunomycin/in
ADP + phosphate + daunomycin/out
-
-
-
-
?
ATP + H2O + daunomycin/in
ADP + phosphate + daunomycin/out
YdaG/YdbA heterodimer
-
-
?
ATP + H2O + daunomycin/in
ADP + phosphate + daunomycin/out
YdaG/YdbA heterodimer
-
-
?
ATP + H2O + daunomycin/in
ADP + phosphate + daunomycin/out
-
-
-
-
?
ATP + H2O + daunorubicin/in
ADP + phosphate + daunorubicin/out
-
-
-
-
?
ATP + H2O + daunorubicin/in
ADP + phosphate + daunorubicin/out
-
-
-
-
?
ATP + H2O + daunorubicin/in
ADP + phosphate + daunorubicin/out
-
-
-
?
ATP + H2O + daunorubicin/in
ADP + phosphate + daunorubicin/out
-
fluorescent substrate of P-glycoprotein
-
-
?
ATP + H2O + daunorubicin/in
ADP + phosphate + daunorubicin/out
-
-
-
-
?
ATP + H2O + daunorubicin[side 1]
ADP + phosphate + daunorubicin[side 2]
-
-
-
-
?
ATP + H2O + daunorubicin[side 1]
ADP + phosphate + daunorubicin[side 2]
-
-
-
-
?
ATP + H2O + daunorubicin[side 1]
ADP + phosphate + daunorubicin[side 2]
-
-
-
?
ATP + H2O + daunorubicin[side 1]
ADP + phosphate + daunorubicin[side 2]
-
-
-
?
ATP + H2O + daunorubicin[side 1]
ADP + phosphate + daunorubicin[side 2]
substrate for BCRP
-
-
?
ATP + H2O + daunorubicin[side 1]
ADP + phosphate + daunorubicin[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + daunorubicin[side 1]
ADP + phosphate + daunorubicin[side 2]
substrate for P-glycoprotein and BCRP
-
-
?
ATP + H2O + diazepam/in
ADP + phosphate + diazepam/out
-
-
-
-
?
ATP + H2O + diazepam/in
ADP + phosphate + diazepam/out
-
-
-
-
?
ATP + H2O + diltiazem/in
ADP + phosphate + diltiazem/out
-
-
-
-
?
ATP + H2O + diltiazem/in
ADP + phosphate + diltiazem/out
-
-
-
-
?
ATP + H2O + diltiazem/in
ADP + phosphate + diltiazem/out
-
-
-
?
ATP + H2O + diltiazem/in
ADP + phosphate + diltiazem/out
-
-
-
-
?
ATP + H2O + diltiazem/in
ADP + phosphate + diltiazem/out
-
-
-
-
?
ATP + H2O + doxorubicin/in
ADP + phosphate + doxorubicin/out
-
-
-
-
?
ATP + H2O + doxorubicin/in
ADP + phosphate + doxorubicin/out
-
-
696714, 697110, 697583, 701435, 711073, 711656, 711932, 712696, 713066, 718864, 733539, 734441 -
-
?
ATP + H2O + doxorubicin/in
ADP + phosphate + doxorubicin/out
-
-
-
?
ATP + H2O + doxorubicin/in
ADP + phosphate + doxorubicin/out
-
-
-
-
?
ATP + H2O + doxorubicin/in
ADP + phosphate + doxorubicin/out
-
-
-
?
ATP + H2O + doxorubicin[side 1]
ADP + phosphate + doxorubicin[side 2]
-
-
-
-
?
ATP + H2O + doxorubicin[side 1]
ADP + phosphate + doxorubicin[side 2]
-
-
-
-
?
ATP + H2O + doxorubicin[side 1]
ADP + phosphate + doxorubicin[side 2]
-
-
-
-
?
ATP + H2O + doxorubicin[side 1]
ADP + phosphate + doxorubicin[side 2]
-
-
-
?
ATP + H2O + doxorubicin[side 1]
ADP + phosphate + doxorubicin[side 2]
-
-
-
?
ATP + H2O + doxorubicin[side 1]
ADP + phosphate + doxorubicin[side 2]
substrate for P-glycoprotein, BCRP, and MPR2
-
-
?
ATP + H2O + doxorubicin[side 1]
ADP + phosphate + doxorubicin[side 2]
substrate for P-glycoprotein, BCRP, and MRP1
-
-
?
ATP + H2O + doxorubicin[side 1]
ADP + phosphate + doxorubicin[side 2]
-
-
-
-
?
ATP + H2O + doxorubicin[side 1]
ADP + phosphate + doxorubicin[side 2]
-
-
-
-
?
ATP + H2O + erythromycin[side 1]
ADP + phosphate + erythromycin[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + erythromycin[side 1]
ADP + phosphate + erythromycin[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + estrone-3-sulfate/in
ADP + phosphate + estrone-3-sulfate/out
-
-
-
-
?
ATP + H2O + estrone-3-sulfate/in
ADP + phosphate + estrone-3-sulfate/out
-
-
-
-
?
ATP + H2O + estrone-3-sulfate[side 1]
ADP + phosphate + estrone-3-sulfate[side 2]
-
-
-
?
ATP + H2O + estrone-3-sulfate[side 1]
ADP + phosphate + estrone-3-sulfate[side 2]
-
-
-
-
?
ATP + H2O + estrone-3-sulfate[side 1]
ADP + phosphate + estrone-3-sulfate[side 2]
substrate for BCRP
-
-
?
ATP + H2O + ethanol/in
ADP + phosphate + ethanol/out
-
-
-
-
?
ATP + H2O + ethanol/in
ADP + phosphate + ethanol/out
-
-
-
-
?
ATP + H2O + ethidium bromide/in
ADP + phosphate + ethidium bromide/out
-
-
-
-
?
ATP + H2O + ethidium bromide/in
ADP + phosphate + ethidium bromide/out
-
recombinant LmrA, expressed in Escherichia coli WD2
-
-
?
ATP + H2O + ethidium bromide/in
ADP + phosphate + ethidium bromide/out
YdaG/YdbA heterodimer
-
-
?
ATP + H2O + ethidium bromide/in
ADP + phosphate + ethidium bromide/out
-
-
-
-
?
ATP + H2O + ethidium bromide/in
ADP + phosphate + ethidium bromide/out
-
-
-
?
ATP + H2O + ethidium bromide[side 1]
ADP + phosphate + ethidium bromide[side 2]
-
-
-
?
ATP + H2O + ethidium bromide[side 1]
ADP + phosphate + ethidium bromide[side 2]
-
-
-
-
?
ATP + H2O + etoposide/in
ADP + phosphate + etoposide/out
-
-
-
-
?
ATP + H2O + etoposide/in
ADP + phosphate + etoposide/out
-
-
-
?
ATP + H2O + etoposide[side 1]
ADP + phosphate + etoposide[side 2]
-
-
-
-
?
ATP + H2O + etoposide[side 1]
ADP + phosphate + etoposide[side 2]
-
-
-
?
ATP + H2O + etoposide[side 1]
ADP + phosphate + etoposide[side 2]
substrate for MRP1
-
-
?
ATP + H2O + etoposide[side 1]
ADP + phosphate + etoposide[side 2]
substrate for P-glycoprotein, BCRP, and MPR2
-
-
?
ATP + H2O + fluconazole/in
ADP + phosphate + fluconazole/out
-
-
-
-
?
ATP + H2O + fluconazole/in
ADP + phosphate + fluconazole/out
-
recombinant Cdr1p
-
-
?
ATP + H2O + fluconazole/in
ADP + phosphate + fluconazole/out
-
-
-
-
?
ATP + H2O + fluoxetine/in
ADP + phosphate + fluoxetine/out
-
-
-
-
?
ATP + H2O + fluoxetine/in
ADP + phosphate + fluoxetine/out
-
-
-
-
?
ATP + H2O + fluvoxamine/in
ADP + phosphate + fluvoxamine/out
-
-
-
-
?
ATP + H2O + fluvoxamine/in
ADP + phosphate + fluvoxamine/out
-
-
-
-
?
ATP + H2O + furosemide/in
ADP + phosphate + furosemide/out
-
-
-
-
?
ATP + H2O + furosemide/in
ADP + phosphate + furosemide/out
-
good substrate for MRP3, but not for MRP1
-
-
?
ATP + H2O + gefitinib[side 1]
ADP + phosphate + gefitinib[side 2]
substrate for BCRP
-
-
?
ATP + H2O + gefitinib[side 1]
ADP + phosphate + gefitinib[side 2]
substrate for P-glycoprotein and BCRP
-
-
?
ATP + H2O + genistein[side 1]
ADP + phosphate + genistein[side 2]
substrate for BCRP
-
-
?
ATP + H2O + genistein[side 1]
ADP + phosphate + genistein[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + Hoechst 33342/in
ADP + phosphate + Hoechst 33342/out
-
-
-
-
?
ATP + H2O + Hoechst 33342/in
ADP + phosphate + Hoechst 33342/out
-
-
-
-
?
ATP + H2O + Hoechst 33342/in
ADP + phosphate + Hoechst 33342/out
-
-
-
-
?
ATP + H2O + Hoechst 33342/in
ADP + phosphate + Hoechst 33342/out
-
-
-
?
ATP + H2O + Hoechst 33342[side 1]
ADP + phosphate + Hoechst 33342[side 2]
-
-
-
-
?
ATP + H2O + Hoechst 33342[side 1]
ADP + phosphate + Hoechst 33342[side 2]
-
-
-
?
ATP + H2O + Hoechst 33342[side 1]
ADP + phosphate + Hoechst 33342[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + Hoechst33342[side 1]
ADP + phosphate + Hoechst33342[side 2]
-
-
-
?
ATP + H2O + Hoechst33342[side 1]
ADP + phosphate + Hoechst33342[side 2]
-
-
-
?
ATP + H2O + Hoechst33342[side 1]
ADP + phosphate + Hoechst33342[side 2]
-
-
-
-
?
ATP + H2O + Hoechst33342[side 1]
ADP + phosphate + Hoechst33342[side 2]
-
-
-
-
?
ATP + H2O + hydroxyzine/in
ADP + phosphate + hydroxyzine/out
-
-
-
-
?
ATP + H2O + hydroxyzine/in
ADP + phosphate + hydroxyzine/out
-
-
-
-
?
ATP + H2O + indinavir[side 1]
ADP + phosphate + indinavir[side 2]
substrate for MPR2
-
-
?
ATP + H2O + indinavir[side 1]
ADP + phosphate + indinavir[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + indinavir[side 1]
ADP + phosphate + indinavir[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + indomethacin/in
ADP + phosphate + indomethacin/out
-
-
-
-
?
ATP + H2O + indomethacin/in
ADP + phosphate + indomethacin/out
-
moderate substrate for MRP1, weak substrate for MRP3
-
-
?
ATP + H2O + iodoarylazidoprazosin[side 1]
ADP + phosphate + iodoarylazidoprazosin[side 2]
-
-
-
?
ATP + H2O + iodoarylazidoprazosin[side 1]
ADP + phosphate + iodoarylazidoprazosin[side 2]
-
-
-
-
?
ATP + H2O + itraconazole/in
ADP + phosphate + itraconazole/out
-
-
-
-
?
ATP + H2O + itraconazole/in
ADP + phosphate + itraconazole/out
-
-
-
-
?
ATP + H2O + ketoconazole/in
ADP + phosphate + ketoconazole/out
-
-
-
-
?
ATP + H2O + ketoconazole/in
ADP + phosphate + ketoconazole/out
-
substrate from a ethyl acetate extract of Trichilia emetica leaves and seeds
-
-
?
ATP + H2O + ketoconazole/in
ADP + phosphate + ketoconazole/out
-
-
-
-
?
ATP + H2O + ketoconazole/in
ADP + phosphate + ketoconazole/out
-
substrate from a ethyl acetate extract of Trichilia emetica leaves and seeds
-
-
?
ATP + H2O + ketoconazole/in
ADP + phosphate + ketoconazole/out
-
substrate from a ethyl acetate extract of Trichilia emetica leaves and seeds
-
-
?
ATP + H2O + ketoconazole/in
ADP + phosphate + ketoconazole/out
-
substrate from a ethyl acetate extract of Trichilia emetica leaves and seeds
-
-
?
ATP + H2O + ketoconazole[side 1]
ADP + phosphate + ketoconazole[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + ketoconazole[side 1]
ADP + phosphate + ketoconazole[side 2]
-
-
-
-
?
ATP + H2O + ketoconazole[side 1]
ADP + phosphate + ketoconazole[side 2]
-
-
-
-
?
ATP + H2O + leukotriene C4/in
ADP + phosphate + leukotriene C4/out
-
high activity with
-
-
?
ATP + H2O + leukotriene C4/in
ADP + phosphate + leukotriene C4/out
-
-
-
-
?
ATP + H2O + leukotriene C4/in
ADP + phosphate + leukotriene C4/out
-
natural substrate of MRP1
-
-
?
ATP + H2O + leukotriene C4/in
ADP + phosphate + leukotriene C4/out
-
natural substrate of MRP1, ATP-stimulated LTC4 uptake of Sf9 inside-out membrane vesicles, roles of the highly conserved ABC-signature regions in the two non-equivalent ABC units of MRP1, major functional role of the conserved glycine residues in both ABC units of MRP1 and formation of composite catalytically active sites involving both signature regions within the ABC domains
-
-
?
ATP + H2O + leukotriene C4/in
ADP + phosphate + leukotriene C4/out
-
glutathione is not required
-
-
?
ATP + H2O + leukotriene C4/in
ADP + phosphate + leukotriene C4/out
-
-
-
-
?
ATP + H2O + loperamide/in
ADP + phosphate + loperamide/out
-
-
-
-
?
ATP + H2O + loperamide/in
ADP + phosphate + loperamide/out
-
-
-
-
?
ATP + H2O + lopinavir[side 1]
ADP + phosphate + lopinavir[side 2]
substrate for MPR2 and BCRP
-
-
?
ATP + H2O + lopinavir[side 1]
ADP + phosphate + lopinavir[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + methotrexate/in
ADP + phosphate + methotrexate/out
-
-
-
-
?
ATP + H2O + methotrexate/in
ADP + phosphate + methotrexate/out
-
-
-
-
?
ATP + H2O + methotrexate/in
ADP + phosphate + methotrexate/out
-
-
-
-
?
ATP + H2O + methotrexate[side 1]
ADP + phosphate + methotrexate[side 2]
-
-
-
?
ATP + H2O + methotrexate[side 1]
ADP + phosphate + methotrexate[side 2]
-
-
-
?
ATP + H2O + methotrexate[side 1]
ADP + phosphate + methotrexate[side 2]
substrate for ABCC4
-
-
?
ATP + H2O + methotrexate[side 1]
ADP + phosphate + methotrexate[side 2]
substrate for ABCG2
-
-
?
ATP + H2O + methotrexate[side 1]
ADP + phosphate + methotrexate[side 2]
substrate for BCRP
-
-
?
ATP + H2O + methotrexate[side 1]
ADP + phosphate + methotrexate[side 2]
substrate for P-glycoprotein, BCRP, and MPR2
-
-
?
ATP + H2O + methotrexate[side 1]
ADP + phosphate + methotrexate[side 2]
-
-
-
?
ATP + H2O + miconazole/in
ADP + phosphate + miconazole/out
-
-
-
-
?
ATP + H2O + miconazole/in
ADP + phosphate + miconazole/out
-
recombinant Cdr1p
-
-
?
ATP + H2O + miconazolenitrate[side 1]
ADP + phosphate + miconazolenitrate[side 2]
-
-
-
-
?
ATP + H2O + miconazolenitrate[side 1]
ADP + phosphate + miconazolenitrate[side 2]
-
-
-
-
?
ATP + H2O + midazolam/in
ADP + phosphate + midazolam/out
-
-
-
-
?
ATP + H2O + midazolam/in
ADP + phosphate + midazolam/out
-
-
-
-
?
ATP + H2O + mitomycin C[side 1]
ADP + phosphate + mitomycin C[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + mitomycin C[side 1]
ADP + phosphate + mitomycin C[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + mitoxantrone[side 1]
ADP + phosphate + mitoxantrone[side 2]
-
-
-
-
?
ATP + H2O + mitoxantrone[side 1]
ADP + phosphate + mitoxantrone[side 2]
-
-
-
?
ATP + H2O + mitoxantrone[side 1]
ADP + phosphate + mitoxantrone[side 2]
substrate for BCRP
-
-
?
ATP + H2O + mitoxantrone[side 1]
ADP + phosphate + mitoxantrone[side 2]
substrate for P-glycoprotein, BCRP, and MPR2
-
-
?
ATP + H2O + N-benzyl-2-nitro-1H-imidazole-1-acetamide/in
ADP + phosphate + N-benzyl-2-nitro-1H-imidazole-1-acetamide/out
-
-
-
-
?
ATP + H2O + N-benzyl-2-nitro-1H-imidazole-1-acetamide/in
ADP + phosphate + N-benzyl-2-nitro-1H-imidazole-1-acetamide/out
-
-
-
-
?
ATP + H2O + N-ethylmaleimide S-glutathione/in
ADP + phosphate + N-ethylmaleimide S-glutathione/out
-
-
-
-
?
ATP + H2O + N-ethylmaleimide S-glutathione/in
ADP + phosphate + N-ethylmaleimide S-glutathione/out
-
NEM-GS is a good substrate for MRP1, but not for MRP3
-
-
?
ATP + H2O + N-ethylmaleimide S-glutathione/in
ADP + phosphate + N-ethylmaleimide S-glutathione/out
-
roles of the highly conserved ABC-signature regions in the two non-equivalent ABC units of MRP1, major functional role of the conserved glycine residues in both ABC units of MRP1 and formation of composite catalytically active sites involving both signature regions within the ABC domains
-
-
?
ATP + H2O + nelfinavir[side 1]
ADP + phosphate + nelfinavir[side 2]
substrate for MPR2 and BCRP
-
-
?
ATP + H2O + nelfinavir[side 1]
ADP + phosphate + nelfinavir[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + norfloxacin[side 1]
ADP + phosphate + norfloxacin[side 2]
-
-
-
-
?
ATP + H2O + norfloxacin[side 1]
ADP + phosphate + norfloxacin[side 2]
substrate for BCRP
-
-
?
ATP + H2O + norfloxacin[side 1]
ADP + phosphate + norfloxacin[side 2]
-
-
-
-
?
ATP + H2O + nortryptiline/in
ADP + phosphate + nortryptiline/out
-
-
-
-
?
ATP + H2O + nortryptiline/in
ADP + phosphate + nortryptiline/out
-
-
-
-
?
ATP + H2O + ochratoxin A[side 1]
ADP + phosphate + ochratoxin A[side 2]
-
-
-
?
ATP + H2O + ochratoxin A[side 1]
ADP + phosphate + ochratoxin A[side 2]
-
-
-
?
ATP + H2O + ofloxacin[side 1]
ADP + phosphate + ofloxacin[side 2]
-
-
-
-
?
ATP + H2O + ofloxacin[side 1]
ADP + phosphate + ofloxacin[side 2]
substrate for BCRP
-
-
?
ATP + H2O + p-methoxy-ethylamphetamine/in
ADP + phosphate + p-methoxy-ethylamphetamine/out
-
-
-
-
?
ATP + H2O + p-methoxy-ethylamphetamine/in
ADP + phosphate + p-methoxy-ethylamphetamine/out
-
-
-
-
?
ATP + H2O + p-methoxy-ethylamphetamine/in
ADP + phosphate + p-methoxy-ethylamphetamine/out
-
cell resistance against the drug substrate is diminished by ATP depletion and enzyme inhibition
-
-
?
ATP + H2O + paclitaxel/in
ADP + phosphate + paclitaxel/out
-
-
-
?
ATP + H2O + paclitaxel/in
ADP + phosphate + paclitaxel/out
-
-
-
-
?
ATP + H2O + paclitaxel/in
ADP + phosphate + paclitaxel/out
-
-
-
?
ATP + H2O + paroxetine/in
ADP + phosphate + paroxetine/out
-
-
-
-
?
ATP + H2O + paroxetine/in
ADP + phosphate + paroxetine/out
-
-
-
-
?
ATP + H2O + prazosin/in
ADP + phosphate + prazosin/out
-
-
-
-
?
ATP + H2O + prazosin/in
ADP + phosphate + prazosin/out
-
-
-
-
?
ATP + H2O + prednisone/in
ADP + phosphate + prednisone/out
-
-
-
-
?
ATP + H2O + prednisone/in
ADP + phosphate + prednisone/out
-
-
-
-
?
ATP + H2O + probenecid/in
ADP + phosphate + probenecid/out
-
-
-
-
?
ATP + H2O + probenecid/in
ADP + phosphate + probenecid/out
-
-
-
-
?
ATP + H2O + progesterone/in
ADP + phosphate + progesterone/out
-
-
-
-
?
ATP + H2O + progesterone/in
ADP + phosphate + progesterone/out
-
-
-
-
?
ATP + H2O + progesterone/in
ADP + phosphate + progesterone/out
-
-
-
-
?
ATP + H2O + progesterone/in
ADP + phosphate + progesterone/out
-
P-gp substrate
-
-
?
ATP + H2O + propoxyphene/in
ADP + phosphate + propoxyphene/out
-
-
-
-
?
ATP + H2O + propoxyphene/in
ADP + phosphate + propoxyphene/out
-
-
-
-
?
ATP + H2O + quercetin[side 1]
ADP + phosphate + quercetin[side 2]
-
-
-
?
ATP + H2O + quercetin[side 1]
ADP + phosphate + quercetin[side 2]
substrate for BCRP
-
-
?
ATP + H2O + quercetin[side 1]
ADP + phosphate + quercetin[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + quinidine/in
ADP + phosphate + quinidine/out
-
-
-
-
?
ATP + H2O + quinidine/in
ADP + phosphate + quinidine/out
-
affinity of qunidine to MDR1 is higher at pH 7.4 than at pH 6.8. Protein concentration is inversely related to the maximum activation of ATPase activity achieved
-
-
?
ATP + H2O + quinidine/in
ADP + phosphate + quinidine/out
-
EC50 value 0.0164 mM
-
-
?
ATP + H2O + quinidine/in
ADP + phosphate + quinidine/out
-
-
-
-
?
ATP + H2O + quinidine[side 1]
ADP + phosphate + quinidine[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + quinidine[side 1]
ADP + phosphate + quinidine[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + quinidine[side 1]
ADP + phosphate + quinidine[side 2]
-
-
-
?
ATP + H2O + rhodamine 123/in
ADP + phosphate + rhodamine 123/out
-
-
-
-
?
ATP + H2O + rhodamine 123/in
ADP + phosphate + rhodamine 123/out
-
less efficient substrate than tetramethylrosamine
-
-
?
ATP + H2O + rhodamine 123/in
ADP + phosphate + rhodamine 123/out
-
-
-
-
?
ATP + H2O + rhodamine 123/in
ADP + phosphate + rhodamine 123/out
-
-
-
?
ATP + H2O + rhodamine 123/in
ADP + phosphate + rhodamine 123/out
-
fluorescent substrate
-
-
?
ATP + H2O + rhodamine 123/in
ADP + phosphate + rhodamine 123/out
-
the enzyme plays an important role in drug resistance
-
-
?
ATP + H2O + rhodamine 123/in
ADP + phosphate + rhodamine 123/out
-
-
-
-
?
ATP + H2O + rhodamine 123/in
ADP + phosphate + rhodamine 123/out
-
-
-
-
?
ATP + H2O + rhodamine 123/in
ADP + phosphate + rhodamine 123/out
-
-
-
-
?
ATP + H2O + rhodamine 123[side 1]
ADP + phosphate + rhodamine 123[side 2]
-
-
-
?
ATP + H2O + rhodamine 123[side 1]
ADP + phosphate + rhodamine 123[side 2]
-
-
-
?
ATP + H2O + rhodamine 123[side 1]
ADP + phosphate + rhodamine 123[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + rhodamine 123[side 1]
ADP + phosphate + rhodamine 123[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + rhodamine 123[side 1]
ADP + phosphate + rhodamine 123[side 2]
-
-
-
?
ATP + H2O + rhodamine 6G/in
ADP + phosphate + rhodamine 6G/out
-
-
-
-
?
ATP + H2O + rhodamine 6G/in
ADP + phosphate + rhodamine 6G/out
-
recombinant Cdr1p
-
-
?
ATP + H2O + rhodamine 6G/in
ADP + phosphate + rhodamine 6G/out
-
-
-
-
?
ATP + H2O + rhodamine 6G/in
ADP + phosphate + rhodamine 6G/out
-
substrate for Snq2p and Pdr5p
-
-
?
ATP + H2O + rhodamine 6G[side 1]
ADP + phosphate + rhodamine 6G[side 2]
-
-
-
?
ATP + H2O + rhodamine 6G[side 1]
ADP + phosphate + rhodamine 6G[side 2]
-
-
-
-
?
ATP + H2O + rhodamine 6G[side 1]
ADP + phosphate + rhodamine 6G[side 2]
-
-
-
-
?
ATP + H2O + riboflavin[side 1]
ADP + phosphate + riboflavin[side 2]
-
-
-
?
ATP + H2O + riboflavin[side 1]
ADP + phosphate + riboflavin[side 2]
substrate for BCRP
-
-
?
ATP + H2O + risperidone/in
ADP + phosphate + risperidone/out
-
-
-
-
?
ATP + H2O + risperidone/in
ADP + phosphate + risperidone/out
-
-
-
-
?
ATP + H2O + ritonavir/in
ADP + phosphate + ritonavir/out
-
-
-
-
?
ATP + H2O + ritonavir/in
ADP + phosphate + ritonavir/out
-
-
-
-
?
ATP + H2O + ritonavir/in
ADP + phosphate + ritonavir/out
-
-
-
-
?
ATP + H2O + ritonavir[side 1]
ADP + phosphate + ritonavir[side 2]
-
-
-
?
ATP + H2O + ritonavir[side 1]
ADP + phosphate + ritonavir[side 2]
substrate for MPR2
-
-
?
ATP + H2O + ritonavir[side 1]
ADP + phosphate + ritonavir[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + ritonavir[side 1]
ADP + phosphate + ritonavir[side 2]
substrate for P-glycoprotein and MRP1
-
-
?
ATP + H2O + ritonavir[side 1]
ADP + phosphate + ritonavir[side 2]
-
-
-
?
ATP + H2O + S-2,4-dinitrophenylglutathione/in
ADP + phosphate + S-2,4-dinitrophenylglutathione/out
-
-
-
-
?
ATP + H2O + S-2,4-dinitrophenylglutathione/in
ADP + phosphate + S-2,4-dinitrophenylglutathione/out
-
-
-
-
?
ATP + H2O + S-2,4-dinitrophenylglutathione/in
ADP + phosphate + S-2,4-dinitrophenylglutathione/out
-
-
-
-
?
ATP + H2O + saquinavir[side 1]
ADP + phosphate + saquinavir[side 2]
-
-
-
?
ATP + H2O + saquinavir[side 1]
ADP + phosphate + saquinavir[side 2]
substrate for MPR2
-
-
?
ATP + H2O + saquinavir[side 1]
ADP + phosphate + saquinavir[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + saquinavir[side 1]
ADP + phosphate + saquinavir[side 2]
-
-
-
?
ATP + H2O + sertraline/in
ADP + phosphate + sertraline/out
-
-
-
-
?
ATP + H2O + sertraline/in
ADP + phosphate + sertraline/out
-
-
-
-
?
ATP + H2O + SN-38[side 1]
ADP + phosphate + SN-38[side 2]
SN-38 is 7-ethyl-10-hydroxy-CPT
-
-
?
ATP + H2O + SN-38[side 1]
ADP + phosphate + SN-38[side 2]
substrate for MPR2 and BCRP
-
-
?
ATP + H2O + tamoxifen[side 1]
ADP + phosphate + tamoxifen[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + tamoxifen[side 1]
ADP + phosphate + tamoxifen[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + teniposide[side 1]
ADP + phosphate + teniposide[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + teniposide[side 1]
ADP + phosphate + teniposide[side 2]
substrate for P-glycoprotein and BCRP
-
-
?
ATP + H2O + tetracycline[side 1]
ADP + phosphate + tetracycline[side 2]
-
-
-
-
?
ATP + H2O + tetracycline[side 1]
ADP + phosphate + tetracycline[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + tetramethylrosamine/in
ADP + phosphate + tetramethylrosamine/out
-
-
-
-
?
ATP + H2O + tetramethylrosamine/in
ADP + phosphate + tetramethylrosamine/out
-
-
-
-
?
ATP + H2O + topotecan[side 1]
ADP + phosphate + topotecan[side 2]
-
-
-
-
?
ATP + H2O + topotecan[side 1]
ADP + phosphate + topotecan[side 2]
-
-
-
?
ATP + H2O + topotecan[side 1]
ADP + phosphate + topotecan[side 2]
substrate for P-glycoprotein and BCRP
-
-
?
ATP + H2O + trans-resveratrol[side 1]
ADP + phosphate + trans-resveratrol[side 2]
-
-
-
?
ATP + H2O + trans-resveratrol[side 1]
ADP + phosphate + trans-resveratrol[side 2]
-
-
-
?
ATP + H2O + trazodone/in
ADP + phosphate + trazodone/out
-
-
-
-
?
ATP + H2O + trazodone/in
ADP + phosphate + trazodone/out
-
-
-
-
?
ATP + H2O + Triton X-100/in
ADP + phosphate + Triton X-100/out
above the critical micellar concentration, Triton X-100 leads to a rapid and irreversible decrease in extracellular acidification rate in both, wild-type and transfected cells which is due to cell lysis
-
-
?
ATP + H2O + Triton X-100/in
ADP + phosphate + Triton X-100/out
-
-
-
-
?
ATP + H2O + Tween 80/in
ADP + phosphate + Tween 80/out
-
-
-
?
ATP + H2O + Tween 80/in
ADP + phosphate + Tween 80/out
-
-
-
-
?
ATP + H2O + urate/in
ADP + phosphate + urate/out
-
-
-
-
?
ATP + H2O + urate/in
ADP + phosphate + urate/out
-
MRP4 is the first secretory transporter identified in the bidirectional renal handling of urate and could be a potential drug target in the treatment of hyperuricaemia, regulation, overview
-
-
?
ATP + H2O + valinomycin/in
ADP + phosphate + valinomycin/out
-
-
-
-
?
ATP + H2O + valinomycin/in
ADP + phosphate + valinomycin/out
-
-
-
-
?
ATP + H2O + verapamil/in
ADP + phosphate + verapamil/out
-
-
-
-
?
ATP + H2O + verapamil/in
ADP + phosphate + verapamil/out
-
-
657840, 685022, 686359, 689695, 697202, 699463, 701069, 701435, 711073, 711894, 711970, 718864, 733332, 733539, 734280, 735307 -
-
?
ATP + H2O + verapamil/in
ADP + phosphate + verapamil/out
-
-
-
?
ATP + H2O + verapamil/in
ADP + phosphate + verapamil/out
-
-
affinity of verapamil to MDR1 is higher at pH 7.4 than at pH 6.8. Protein concentration is inversely related to the maximum activation of ATPase activity achieved
-
?
ATP + H2O + verapamil/in
ADP + phosphate + verapamil/out
-
-
EC50 value 0.00285 mM
-
?
ATP + H2O + verapamil/in
ADP + phosphate + verapamil/out
-
EPR spin-labeled verapamil is an excellent transport substrate, the affinity is 10fold higher than for unlabeled verapamil
-
-
?
ATP + H2O + verapamil/in
ADP + phosphate + verapamil/out
-
P-gp substrate
-
-
?
ATP + H2O + verapamil/in
ADP + phosphate + verapamil/out
-
unlabeled and spin-labeled verapamil
-
-
?
ATP + H2O + verapamil/in
ADP + phosphate + verapamil/out
-
-
-
-
?
ATP + H2O + verapamil/in
ADP + phosphate + verapamil/out
-
-
-
-
?
ATP + H2O + verapamil/in
ADP + phosphate + verapamil/out
-
-
-
-
?
ATP + H2O + verapamil/in
ADP + phosphate + verapamil/out
-
-
-
?
ATP + H2O + verapamil/in
ADP + phosphate + verapamil/out
-
-
-
-
?
ATP + H2O + verapamil/in
ADP + phosphate + verapamil/out
-
-
-
-
?
ATP + H2O + verapamil[side 1]
ADP + phosphate + verapamil[side 2]
-
-
-
?
ATP + H2O + verapamil[side 1]
ADP + phosphate + verapamil[side 2]
-
-
-
-
?
ATP + H2O + verapamil[side 1]
ADP + phosphate + verapamil[side 2]
-
-
-
?
ATP + H2O + verapamil[side 1]
ADP + phosphate + verapamil[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + verapamil[side 1]
ADP + phosphate + verapamil[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + verapamil[side 1]
ADP + phosphate + verapamil[side 2]
-
-
-
?
ATP + H2O + verapamil[side 1]
ADP + phosphate + verapamil[side 2]
-
-
-
-
?
ATP + H2O + vinblastine/in
ADP + phosphate + vinblastine/out
-
-
-
-
?
ATP + H2O + vinblastine/in
ADP + phosphate + vinblastine/out
-
-
659295, 684962, 685450, 696343, 696714, 697760, 699463, 711970, 713202, 718864, 734442 -
-
?
ATP + H2O + vinblastine/in
ADP + phosphate + vinblastine/out
-
-
-
-
?
ATP + H2O + vinblastine/in
ADP + phosphate + vinblastine/out
-
-
-
-
?
ATP + H2O + vinblastine/in
ADP + phosphate + vinblastine/out
-
-
-
-
?
ATP + H2O + vinblastine/in
ADP + phosphate + vinblastine/out
-
-
-
?
ATP + H2O + vinblastine[side 1]
ADP + phosphate + vinblastine[side 2]
-
-
-
?
ATP + H2O + vinblastine[side 1]
ADP + phosphate + vinblastine[side 2]
-
-
-
?
ATP + H2O + vinblastine[side 1]
ADP + phosphate + vinblastine[side 2]
-
-
-
?
ATP + H2O + vinblastine[side 1]
ADP + phosphate + vinblastine[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + vinblastine[side 1]
ADP + phosphate + vinblastine[side 2]
substrate for P-glycoprotein and MPR2
-
-
?
ATP + H2O + vinblastine[side 1]
ADP + phosphate + vinblastine[side 2]
-
-
-
?
ATP + H2O + vinblastine[side 1]
ADP + phosphate + vinblastine[side 2]
-
-
-
-
?
ATP + H2O + vincristine[side 1]
ADP + phosphate + vincristine[side 2]
-
-
-
?
ATP + H2O + vincristine[side 1]
ADP + phosphate + vincristine[side 2]
substrate for P-glycoprotein
-
-
?
ATP + H2O + vincristine[side 1]
ADP + phosphate + vincristine[side 2]
substrate for P-glycoprotein and MPR2
-
-
?
ATP + H2O + VP-16/in
ADP + phosphate + VP-16/out
-
-
-
-
?
ATP + H2O + VP-16/in
ADP + phosphate + VP-16/out
-
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
-
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
multidrug ABC transporter YvcC, the high ATP hydrolysis proceeds via a positive cooperativity mechanism, two drug binding sites coexist on YvcC
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
the enzyme forms stable, highly ordered ring-shaped structures, that are destroyed or whose formation is prevented upon addition of ATP in the presence of Mg2+ and the subsequent catalytic step responsible for such an effect, overview
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
-
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
ABC multidrug transporter Cdr1p, domain structure, roles of Cys-193 of the Walker A motif of the N-terminal nucleotide binding domain and of Lys-901 of the Walker A motif of the C-terminal nucleotide binding domain in ATPase function, the two nucleotide binding domains influence the Cdr1p function asymmetrically
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
importance of Candida drug resistance protein Cdr1p of pathogenic Candida albicans in azole resistance
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
the typical Cys193 in Walker A as well as Trp326 and Asp327 in the Walker B of N-terminal nucleotide binding domain of Cdr1p have acquired unique roles in ATP binding and hydrolysis. Asn328 is a gamma-phosphate sensor. ATP docking subsequent to Mg2+ coordination induces further conformational changes, structure analysis, overview
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
-
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
-
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
-
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
thermodynamic analysis of ATP hydrolysis in the presence and absence of transport substrates, mechanism
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
expression at the tumor cell surface of P-glycoprotein, which functions as an ATP-powered multidrug efflux pump, is involved in multidrug resistance. It also shows lipid flippase activity
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
-
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
-
695397, 696343, 697106, 697110, 697202, 697586, 697760, 697766, 699450, 699463, 699712, 700297, 701069, 701356, 701435, 733539, 734442 -
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
ATP-driven pumping of a variety of drugs out of cells, multidrug resistance, hydrophobic model of drug transport by P-glycoprotein
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
MDR1, multiple drug resistance, ABC transporter, which acts as ATP-driven pump that removes xenobiotics from the interior of cells
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
multidrug resistance, the major physiological role is the protection of cells and tissues against xenobiotics, relevance of MRP1 and MRP3 proteins in chemoresistance of cancer and in drug metabolism and toxicity
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
ATP-driven pumping of a variety of drugs out of cells, hydrophobic vacuum cleaner model of drug transport by P-glycoprotein
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
MDR1, ABC transporter, which acts as ATP-driven pump that removes xenobiotics from the interior of cells, uses a wide variety of substrates
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
mechanism, model of the MRP1 ATPase hydrolytic cycle, nucleotide-binding and MRP1 interaction with the transported substrates induce two different allosteric effects during the ATPase cycle, MRP1 domain structure
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
P-gp catalyzes the ATP hydrolysis-dependent efflux of numerous amphiphilic compounds of unrelated chemical structures
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
Pgp transports drugs out of cells, very broad specificity drug pump, thermodynamic analysis of ATP hydrolysis in the presence and absence of transport substrates, mechanism, model of drug transport
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
wide substrate specificity of MDR proteins, MDR1 preferentially extrudes large hydrophobic, positively charged molecules, members of the MRP family extrudes both hydrophobic uncharged molecules and water-soluble anionic compounds
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
structure-activity relationship, overview
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
MRP1 transports a wide range of natural product drugs and structurally diverse conjugated and unconjugated organic anions. Its closest relative is MRP3. MRP1 transports GSH and GSH conjugates and displays GSH-stimulated transport of a number of unconjugated and conjugated compounds. In contrast, MRP3 does not transport GSH and is a poor transporter of GSH conjugates
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
MRP4 limits brain entry and promotes renal excretion of drugs. In addition to its role in the body distribution and renal excretion of a wide variety of antiviral, cytostatic, antibiotic and cardiovascular drugs, MRP4/ABCC4 has the ability to transport molecules involved in cellular signalling. These molecules include cyclic nucleotides, eicosanoids, urate and conjugated steroids. The unique structure, regulation and dual localisation of MRP4 in polarised cells could be connected with a key function in cellular protection and extracellular signalling pathways, overview
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
multidrug resistance protein MDR1, i.e. P-glycoprotein or ABCB1, is an ATP-dependent efflux pump for various cytotoxic agents, and is implicated in the resistance of human tumors to chemotherapeutic drugs
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
P-glycoprotein belongs to the family of ATP-binding cassette proteins which hydrolyze ATP to catalyse the translocation of their substrates through membranes
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
P-glycoprotein is a membrane ATP-driven drug exporter, Pgp actively extrudes a spectrum of hydrophobic xenobiotics, including a number of anticancer drugs
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
P-gp 170 has two potentially interesting regions for drugs interfering with its efflux function, namely the oligosaccharides on the first extracellular loop with unknown function and the two intracellular ATP-binding regions providing the energy for drug efflux function. P-gp is a polytopic plasma membrane protein whose overexpression causes multidrug resistance, MDR, responsible for the failure of cancer chemotherapy
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
the ATP-binding cassette multidrug resistance protein 1 mediates ATP-dependent cellular efflux of drugs and organic anions
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
the enzyme increases the resistance level of cells against drugs, overview
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
the P-glycoprotein mediates multidrug resistance, which can be overcome by enzyme inhibition and ATP depletion allowing drug containing nanoparticles to target both drug and biological mechanisms
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
a cluster of aromatic residues located at the interface between the nucleotide binding domain and the transmembrane domain in opposite halves of the molecule may contribute to this signal transmission upon ATP binding and hydrolysis, binding and/or hydrolysis of ATP induce conformational changes that are transmitted from the nucleotide binding domains to the transmembrane domains, overview
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
ATP-dependent MRP1-mediated uptake of labeled substrates in membrane vesicles
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
ATP-dependent transport into inside-out membrane vesicles by recombinant enzymes, overview
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
functional importance of MRP1-Pro1150 at the interface of transmembrane helix 15 and cytoplasmic loop 7
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
ABC multidrug transporter LmrA, substrate specificity
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
YdaG and YdbA are two ABC multidrug half-transporters, ATPase activity is associated with the YdaG/YdbA heterodimer only and not with the individual subunits
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
YdaG and YdbA are two ABC multidrug half-transporters, ATPase activity is associated with the YdaG/YdbA heterodimer only and not with the individual subunits
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
ABC multidrug transporter LmrA, substrate specificity
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
-
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
-
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
in the brain, MRP4 limits the entry of drugs and is involved in nociception, probably as a result of reduced plasma prostaglandins. In the kidney, MRP4 mediates the active tubular secretion of diuretics, antiviral nucleosides and cephalosporins. In the liver, MRP4 mediates the efflux of bile acid to the blood, and knockout mice are more sensitive to cholestatic-induced liver injury. MRP4 protects bone marrow cells and the gastrointestinal tract against cytotoxic drugs and appears to be involved in secretory diarrhoea via coupling with CFTR
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
-
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
-
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
-
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
-
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
SMDR2 is an ATP-dependent efflux pump involved in transport of toxins and xenobiotics from cells
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
-
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
-
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
-
-
-
?
ATP + H2O + xenobiotic/in
ADP + phosphate + xenobiotic/out
-
-
-
-
?
ATP + H2O + xenobiotic[side 1]
ADP + phosphate + xenobiotic[side 2]
-
-
-
-
?
ATP + H2O + xenobiotic[side 1]
ADP + phosphate + xenobiotic[side 2]
-
-
-
?
ATP + H2O + xenobiotic[side 1]
ADP + phosphate + xenobiotic[side 2]
-
-
-
?
ATP + H2O + xenobiotic[side 1]
ADP + phosphate + xenobiotic[side 2]
-
-
-
-
?
ATP + H2O + xenobiotic[side 1]
ADP + phosphate + xenobiotic[side 2]
-
-
-
-
?
ATP + H2O + xenobiotic[side 1]
ADP + phosphate + xenobiotic[side 2]
-
-
-
?
ATP + H2O + xenobiotic[side 1]
ADP + phosphate + xenobiotic[side 2]
-
-
-
-
?
ATP + H2O + xenobiotic[side 1]
ADP + phosphate + xenobiotic[side 2]
-
-
-
?
ATP + H2O + xenobiotic[side 1]
ADP + phosphate + xenobiotic[side 2]
-
-
-
?
ATP + H2O + xenobiotic[side 1]
ADP + phosphate + xenobiotic[side 2]
-
-
-
?
ATP + H2O + xenobiotic[side 1]
ADP + phosphate + xenobiotic[side 2]
-
-
-
?
ATP + H2O + xenobiotic[side 1]
ADP + phosphate + xenobiotic[side 2]
-
-
-
-
?
ATP + H2O + xenobiotic[side 1]
ADP + phosphate + xenobiotic[side 2]
-
-
-
?
ATP + H2O + xenobiotic[side 1]
ADP + phosphate + xenobiotic[side 2]
-
-
-
-
?
ATP + H2O + xenobiotic[side 1]
ADP + phosphate + xenobiotic[side 2]
-
-
-
?
ATP + H2O + xenobiotic[side 1]
ADP + phosphate + xenobiotic[side 2]
-
-
-
-
?
ATP + H2O + xenobiotic[side 1]
ADP + phosphate + xenobiotic[side 2]
-
-
-
?
ATP + H2O + xenobiotic[side 1]
ADP + phosphate + xenobiotic[side 2]
-
-
-
-
?
ATP + H2O + xenobiotic[side 1]
ADP + phosphate + xenobiotic[side 2]
-
-
-
?
ATP + H2O + xenobiotic[side 1]
ADP + phosphate + xenobiotic[side 2]
-
-
-
-
?
ATP + H2O + xenobiotic[side 1]
ADP + phosphate + xenobiotic[side 2]
-
-
-
-
?
ATP + H2O + zolpidem/in
ADP + phosphate + zolpidem/out
-
-
-
-
?
ATP + H2O + zolpidem/in
ADP + phosphate + zolpidem/out
-
-
-
-
?
cyclo(D-Trp-D-Asp-L-Pro-D-Val-L-Leu)/in + ATP + H2O
cyclo(D-Trp-D-Asp-L-Pro-D-Val-L-Leu)/out + ADP + phosphate
-
no other common substrate detected
-
?
cyclo(D-Trp-D-Asp-L-Pro-D-Val-L-Leu)/in + ATP + H2O
cyclo(D-Trp-D-Asp-L-Pro-D-Val-L-Leu)/out + ADP + phosphate
-
no other common substrate detected
-
?
daunorubicin/in + ATP + H2O
daunorubicin/out + ADP + phosphate
-
-
-
-
?
daunorubicin/in + ATP + H2O
daunorubicin/out + ADP + phosphate
-
-
-
-
?
doxorubicin/in + ATP + H2O
doxorubicin/out + ADP + phosphate
-
-
-
?
doxorubicin/in + ATP + H2O
doxorubicin/out + ADP + phosphate
-
-
-
?
doxorubicin/in + ATP + H2O
doxorubicin/out + ADP + phosphate
-
-
-
?
doxorubicin/in + ATP + H2O
doxorubicin/out + ADP + phosphate
-
-
-
?
erythromycin/in + ATP + H2O
erythromycin/out + ADP + phosphate
-
-
-
?
erythromycin/in + ATP + H2O
erythromycin/out + ADP + phosphate
-
-
-
?
estradiol 17-beta-D-glucuronide/in + ATP + H2O
estradiol 17-beta-D-glucuronide/out + ADP + phosphate
-
-
-
-
?
estradiol 17-beta-D-glucuronide/in + ATP + H2O
estradiol 17-beta-D-glucuronide/out + ADP + phosphate
-
-
-
?
estradiol 17-beta-D-glucuronide/in + ATP + H2O
estradiol 17-beta-D-glucuronide/out + ADP + phosphate
-
-
-
-
?
etoposide/in + ATP + H2O
etoposide/out + ADP + phosphate
-
-
-
?
etoposide/in + ATP + H2O
etoposide/out + ADP + phosphate
-
-
-
?
etoposide/in + ATP + H2O
etoposide/out + ADP + phosphate
-
-
-
?
GTP + H2O
GDP + phosphate
-
-
-
-
?
GTP + H2O
GDP + phosphate
-
-
-
-
?
leukotriene C4/in + ATP + H2O
leukotriene C4/out + ADP + phosphate
-
-
-
?
leukotriene C4/in + ATP + H2O
leukotriene C4/out + ADP + phosphate
-
-
-
?
leukotriene C4/in + ATP + H2O
leukotriene C4/out + ADP + phosphate
-
-
-
?
leukotriene C4/in + ATP + H2O
leukotriene C4/out + ADP + phosphate
-
-
-
?
leukotriene C4/in + ATP + H2O
leukotriene C4/out + ADP + phosphate
-
-
-
?
leukotriene C4/in + ATP + H2O
leukotriene C4/out + ADP + phosphate
-
-
-
?
leukotriene C4/in + ATP + H2O
leukotriene C4/out + ADP + phosphate
-
-
-
?
leukotriene C4/in + ATP + H2O
leukotriene C4/out + ADP + phosphate
-
-
-
?
leukotriene D4/in + ATP + H2O
leukotriene D4/out + ADP + phosphate
-
-
-
-
?
leukotriene D4/in + ATP + H2O
leukotriene D4/out + ADP + phosphate
-
-
-
-
?
oleandomycin/in + ATP + H2O
oleandomycin/out + ADP + phosphate
-
-
-
?
oleandomycin/in + ATP + H2O
oleandomycin/out + ADP + phosphate
-
-
-
?
rhodamine 123/in + ATP + H2O
rhodamine 123/out + ADP + phosphate
-
-
-
?
rhodamine 123/in + ATP + H2O
rhodamine 123/out + ADP + phosphate
-
-
-
-
?
S-(2,4-dinitrophenyl)glutathione/in + ATP + H2O
S-(2,4-dinitrophenyl)glutathione/out + ADP + phosphate
-
-
-
-
?
S-(2,4-dinitrophenyl)glutathione/in + ATP + H2O
S-(2,4-dinitrophenyl)glutathione/out + ADP + phosphate
-
-
-
-
?
spiramycin/in + ATP + H2O
spiramycin/out + ADP + phosphate
-
-
-
?
spiramycin/in + ATP + H2O
spiramycin/out + ADP + phosphate
-
-
-
?
tetracyclin/in + ATP + H2O
tetracyclin/out + ADP + phosphate
-
-
-
?
tetracyclin/in + ATP + H2O
tetracyclin/out + ADP + phosphate
-
-
-
?
UTP + H2O
UDP + phosphate
-
-
-
-
?
UTP + H2O
UDP + phosphate
-
-
-
-
?
vinblastine/in + ATP + H2O
vinblastine/out + ADP + phosphate
-
-
-
-
?
vinblastine/in + ATP + H2O
vinblastine/out + ADP + phosphate
-
weak activity
-
?
vincristine/in + ATP + H2O
vincristine/out + ADP + phosphate
-
-
-
?
vincristine/in + ATP + H2O
vincristine/out + ADP + phosphate
-
-
-
?
vincristine/in + ATP + H2O
vincristine/out + ADP + phosphate
-
-
-
-
?
vincristine/in + ATP + H2O
vincristine/out + ADP + phosphate
-
-
cotransport with reduced glutathione
?
vincristine/in + ATP + H2O
vincristine/out + ADP + phosphate
-
requires cotransport of GSH
-
?
vincristine/in + ATP + H2O
vincristine/out + ADP + phosphate
-
requires cotransport of GSH
-
?
vincristine/in + ATP + H2O
vincristine/out + ADP + phosphate
-
-
-
?
vincristine/in + ATP + H2O
vincristine/out + ADP + phosphate
-
-
-
?
vincristine/in + ATP + H2O
vincristine/out + ADP + phosphate
-
-
-
?
additional information
?
-
-
transcription of the atrA and the atrB gene is strongly enhanced by treatment with several fungicides and plant defense toxins
-
-
?
additional information
?
-
-
BmrA is a half-ABC transporter involved in multidrug resistance
-
-
?
additional information
?
-
-
multidrug ABC transporter YvcC involved in multidrug resistance, the yvcC gene is constitutively expressed in Bacillus subtilis throughout its growth, the in vivo function is related to a protective role, the MDR pump might act as a housekeeping transporter to quickly cope with the presence of low levels of deleterious compounds, then, if the concentration of these compounds rose above a threshold limit, the expression of additional pumps could be turned on
-
-
?
additional information
?
-
-
no hydrolysis of 5-adenylyl imidodiphosphate, study of YvcC interaction with different drugs
-
-
?
additional information
?
-
-
enzyme plays an important role in microbial resistance to neutral or positively charged amphiphilic drugs
-
-
?
additional information
?
-
-
the recombinant enzyme in Saccharomyces cerevisiae is able to detoxify extracts of diverse plants collected in Mozambique, detailed overview
-
-
?
additional information
?
-
-
the recombinant enzyme in Saccharomyces cerevisiae is able to detoxify extracts of diverse plants collected in Mozambique, detailed overview
-
-
?
additional information
?
-
-
the P-glycoprotein contains two distinct sites for drug binding and transport, these sites interact in a positively cooperative manner
-
-
?
additional information
?
-
-
multidrug transporter, ATP-driven drug transport, the intimate association of both Pgp and its substrates with the membrane suggests that its function may be regulated by the biophysical properties of the lipid bilayer
-
-
?
additional information
?
-
-
the Pgp multidrug transporter carries out ATP-driven cellular efflux of a wide variety of hydrophobic drugs, natural products and peptides
-
-
?
additional information
?
-
-
the fly enzyme exhibits a unique high level basal ATPase activity that is inhibited by the transported substrates, and it is capable of transporting several human MRP substrates like beta-estradiol 17-beta-D-glucuronide, leukotriene C4, calcein, fluo3 and carboxydichlorofluorescein
-
-
?
additional information
?
-
-
enzyme plays an important role in microbial resistance to neutral or positively charged amphiphilic drugs
-
-
?
additional information
?
-
-
the enzyme could cleave phosphoester bonds effectively from a broad range of substrates such as ATP, AMP, p-nitrophenylphosphate and beta-glycerophosphate
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
-
the enzyme operates in an alternating sites mechanism, that is when one catalytic site enters the transition state, the other is unable to do so
-
-
?
additional information
?
-
-
energy-dependent drug efflux pump
-
-
?
additional information
?
-
-
MRP3 is competent in the transport of glutathione S-conjugates, glucuronides and methotrexate, the enzyme is active in the transport of monoanionic human bile constituent glycocholate
-
-
?
additional information
?
-
-
enzyme confers cellular resistance to a variety of natural product cytotoxic agents
-
-
?
additional information
?
-
-
the deficient expression of cMRP appears as the basis of the transport defect in human Dubin-Johnson syndrome
-
-
?
additional information
?
-
-
potential protective role for the enzyme in chemical carcinogenesis
-
-
?
additional information
?
-
-
the physiological function can range from a protective role in chemical toxicity and oxidative stress to mediation of inflammatory responses involving cysteinyl leukotrienes
-
-
?
additional information
?
-
-
MRP5 might play a role in some cases of unexplained resistance to thiopurines in acute lymphoblastic leukemia and/or antiretroviral nucleoside analogs in HIV-infected patients
-
-
?
additional information
?
-
-
MRP1 is an efflux pump, which can transport conjugated organic anions and cotansport vincristine together with GSH
-
-
?
additional information
?
-
-
exports a diverse group of natural products chemotherapeutic drugs, and hydrophobic peptides across the plasma membrane
-
-
?
additional information
?
-
-
overexpression of the multidrug resistance P-glycoprotein and the multidrug resistance-associated protein MRP1 is a principal cause of resistance of cancer to chemotherapy
-
-
?
additional information
?
-
-
MRP1 is a key multidrug resistance ABC transporter in tumor cells
-
-
?
additional information
?
-
-
Pgp transports drugs out of cells
-
-
?
additional information
?
-
-
the ABC transporter MRP1 is involved in the cellular extrusion of conjugated metabolites and causes multidrug resistance in tumor cells
-
-
?
additional information
?
-
-
the ABC transporter P-glycoprotein is responsible for multidrug resistance in tumor cells
-
-
?
additional information
?
-
-
ATPase activity associated with P-glycoprotein is characterized by three drug-dependent phases: basal without drug, drug-activated, and drug-inhibited, the basal ATPase activity is not a consequence of transport of an endogenous lipid or other substrate, but rather an intrinsic mechanistic property of enzyme
-
-
?
additional information
?
-
-
benzbromarone and MK571 may be potential transported substrates for MRP3
-
-
?
additional information
?
-
-
not: desloratadine
-
-
?
additional information
?
-
-
binding of drugs to Pgp is not compatible with a classical key-lock or one-pharmacophore model but can be well explained with a modular binding concept, where the energetically most relevant binding module seems to consist of two hydrogen bond acceptor groups
-
-
?
additional information
?
-
-
the drug substrate binding site of isoform MDR1/P-glycoprotein may best fit to drugs with a molecular mass of between 800 and 900 Da, and cholesterol may support the recognition of smaller drugs by adjusting the drug-binding site
-
-
?
additional information
?
-
-
no substrate: loratidine
-
-
?
additional information
?
-
-
MRP1 is a primary active transporter of conjugated metabolites and endogenous organic anions including leukotriene C4 and glutathione. Enzyme mutations can lead to diabetes mellitus
-
-
?
additional information
?
-
-
MRP5 plays a role in the ocular drug efflux and conferring ocular drug resistance
-
-
?
additional information
?
-
-
stimulation of elimination via MRP2 may result in suboptimal chemotherapeutic drug concentrations, and stimulation of MRP2 activity in tumors may lead to increased efflux of chemotherapeutic drugs and thereby drug resistance
-
-
?
additional information
?
-
-
substrate specificity, overview. Renal excretion is an important route of elimination for many MRP4 substrates. MRP4 has a putative pathophysiological function in signalling, and it protects the liver from accumulation of toxic bile acids during cholestasis by facilitating their efflux into blood for ultimate renal excretion
-
-
?
additional information
?
-
-
the intrinsic multidrug resistance, MDR, of cholangiocellular and gallbladder carcinomas seems to be independent of MRP2 expression while the expression of MRP3 may contribute to the MDR phenotype
-
-
?
additional information
?
-
-
The polylactoseamine oligosaccharides on the first loop of P-gp 170 can specifically bind the tomato lectin which possibly stabilizes the functional active conformation of P-gp
-
-
?
additional information
?
-
-
enzyme molecular modeling, overview
-
-
?
additional information
?
-
-
ligand binding structure analysis using the three-dimensional structure modelling, overview
-
-
?
additional information
?
-
-
MRP7 has a broad resistance profile for natural products, no transport activity with nontaxane antimicrotubule agents
-
-
?
additional information
?
-
-
P-glycoprotein seems to prefer amphipathic cationic compounds, and MRP1 anionic compounds
-
-
?
additional information
?
-
-
Pgp transport studies across recombinant MDCK-MDR1 monolayers, overview
-
-
?
additional information
?
-
-
Tyr440, naturally occuring in wild-type MRP3 and recombinantly in MRP1 mutants, makes a major contribution to recognition of GSH and the GSH moiety of conjugates such as LTC4
-
-
?
additional information
?
-
-
the human multidrug resistance transporter P-glycoprotein prevents the entry of compounds into the brain by an active efflux mechanism at the blood-brain barrier
-
-
?
additional information
?
-
-
P-gp possesses a linker region of about 75 amino acids that connects two homologous halves, each of which contain a transmembrane domain followed by a nucleotide-binding domain. The linker region regulates the inherent substrate specificity of P-gp
-
-
?
additional information
?
-
tested compounds exhibiting similar influx as efflux induce different ATPase activity profiles in cells and inside-out vesicles. Their concentration is significantly lower in the cytosolic leaflet of cells than in the cytosolic leaflet of inside-out membrane vesicles, indicating that P-glycoprotein can cope with passive influx. P-glycoprotein thus transports all compounds tested at a rate proportional to ATP hydrolysis. However, it prevents substrate entry into the cytosol only if passive influx of substrates across the lipid bilayer is in a similar range as active efflux
-
-
?
additional information
?
-
n-dodecyl-beta-D-maltoside is no substrate for the enzyme, and the presence of n-dodecyl-beta-D-maltoside does not alter the locations of drug-binding sites, e.g. for tariquidar. The enzyme shows drug-stimulated ATPase activity
-
-
-
additional information
?
-
-
n-dodecyl-beta-D-maltoside is no substrate for the enzyme, and the presence of n-dodecyl-beta-D-maltoside does not alter the locations of drug-binding sites, e.g. for tariquidar. The enzyme shows drug-stimulated ATPase activity
-
-
-
additional information
?
-
-
possible role for LmrA in lipid trafficking
-
-
?
additional information
?
-
role of the YdaG/YdbA heterodimer in drug resistance
-
-
?
additional information
?
-
-
role of the YdaG/YdbA heterodimer in drug resistance
-
-
?
additional information
?
-
-
LmrA and the lipid transporter MsbA in Escherichia coli have overlapping specificities for Lipid A and chemotherapeutic and cytotoxic drugs
-
-
?
additional information
?
-
role of the YdaG/YdbA heterodimer in drug resistance
-
-
?
additional information
?
-
-
possible role for LmrA in lipid trafficking
-
-
?
additional information
?
-
-
LmrA and the lipid transporter MsbA in Escherichia coli have overlapping specificities for Lipid A and chemotherapeutic and cytotoxic drugs
-
-
?
additional information
?
-
-
enzyme plays an important role in microbial resistance to neutral or positively charged amphiphilic drugs
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
-
the enzyme functions as cotransporter of glutathione and natural product toxins
-
-
?
additional information
?
-
-
energy-dependent drug efflux pump
-
-
?
additional information
?
-
-
baseline enzyme expression protects cells from the toxic effects of xenobiotics by effluxing the xenobiotics and GSH from the intracellular compartment into the extracellular medium by a cotransport mechanism
-
-
?
additional information
?
-
-
the enzyme in the canalicular membrane plays an important role in the excretion of phospholipid into bile
-
-
?
additional information
?
-
-
no substrate: loratidine
-
-
?
additional information
?
-
-
MRP5 plays a role in the ocular drug efflux lowering the permeability of antiviral and glaucoma drugs and conferring ocular drug resistance
-
-
?
additional information
?
-
-
enzyme plays an important role in microbial resistance to neutral or positively charged amphiphilic drugs
-
-
?
additional information
?
-
-
Pgh1 is not involved as a chloroquine transporter in the plasma membrane of Plasmodium falciparum
-
-
?
additional information
?
-
-
substrate comparison between fish P-glycoprotein and human P-glycoprotein, identification of five compounds that specifically interact only with fish P-glycoprotein, while seven compounds exhibit specific interaction only with human P-glycoprotein. Sixteen tested compounds show interaction with both proteins, and there is significant correlation in the interaction potency between fish and human P-glycoprotein for those compounds that interact with both proteins
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
-
no transport of endothelin I and Arg8-vasopressin by MRP6
-
-
?
additional information
?
-
-
phosphatidylinositol 3-kinase activity is necessary for maximal ATP-dependent transport of taurocholate and dinitrophenyl-glutathione in vivo. Type I phosphatidylinositol 3-kinase lipid products directly regulate ATP-dependent membrane transport system and function of ATP binding cassette membrane proteins
-
-
?
additional information
?
-
-
does not play a major role in canalicular organic anion excretion. The enzyme might fulfill a housekeeping transport function involved in the regulation of paracellular and/or transcellular solute movement from blood into bile
-
-
?
additional information
?
-
-
no transport of endothelin I and Arg8-vasopressin by MRP6
-
-
?
additional information
?
-
-
does not play a major role in canalicular organic anion excretion. The enzyme might fulfill a housekeeping transport function involved in the regulation of paracellular and/or transcellular solute movement from blood into bile
-
-
?
additional information
?
-
-
adult worms from the Egyptian Schistosoma mansoni isolate with reduced sensitivity to praziquantel express increased levels of SMDR2
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additional information
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subunit DrrA of DrrAB hydrolyzes ATP, and the energy is transduced to carrier DrrB resulting in export of drugs
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additional information
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the recombinant enzyme in Saccharomyces cerevisiae is able to detoxify extracts of diverse plants collected in Mozambique, detailed overview
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additional information
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the recombinant enzyme in Saccharomyces cerevisiae is able to detoxify extracts of diverse plants collected in Mozambique, detailed overview
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(17beta)-N-([trans-4-[(6-amino-9H-purin-9-yl)methyl]cyclohexyl]methyl)-3-oxoandrost-4-ene-17-carboxamide
-
daunorubicin accumulation is 99% of the accumulation in presence of 0.01 mM progesterone
(17beta)-N-[(2E)-4-(6-amino-9H-purin-9-yl)but-2-en-1-yl]-3-oxoandrost-4-ene-17-carboxamide
-
daunorubicin accumulation is 72% of the accumulation in presence of 0.01 mM progesterone
(17beta)-N-[(2Z)-4-(6-amino-9H-purin-9-yl)but-2-en-1-yl]-3-oxoandrost-4-ene-17-carboxamide
-
daunorubicin accumulation is 86% of the accumulation in presence of 0.01 mM progesterone
(17beta)-N-[4-(6-amino-9H-purin-9-yl)but-2-yn-1-yl]-3-oxoandrost-4-ene-17-carboxamide
-
daunorubicin accumulation is 61% of the accumulation in presence of 0.01 mM progesterone
(17beta)-N-[4-(6-amino-9H-purin-9-yl)butyl]-3-oxoandrost-4-ene-17-carboxamide
-
daunorubicin accumulation is 78% of the accumulation in presence of 0.01 mM progesterone
(17beta)-N-[4-[(6-amino-9H-purin-9-yl)methyl]benzyl]-3-oxoandrost-4-ene-17-carboxamide
-
daunorubicin accumulation is 98% of the accumulation in presence of 0.01 mM progesterone
(17beta)-N-[6-(6-amino-9H-purin-9-yl)hexyl]-3-oxoandrost-4-ene-17-carboxamide
-
daunorubicin accumulation is 111% of the accumulation in presence of 0.01 mM progesterone
(1beta,1'beta)-5-bromo-6,6',7,12-tetramethoxy-2-methylberbaman
-
is an effectively and potential agent in reversing Pgp-mediated multidrug resistance by inhibiting the transport function and expression of Pgp
(1E)-1,5-bis[3,5-bis(methoxymethoxy)phenyl]-4,4-dibromopent-1-en-3-one
58.7% inhibition at 0.01 mM
(1E)-1,5-bis[3,5-bis(methoxymethoxy)phenyl]-4,4-dichloropent-1-en-3-one
51.5% inhibition at 0.01 mM
(1E)-1,5-bis[3,5-bis(methoxymethoxy)phenyl]-4,4-difluoropent-1-en-3-one
44.4% inhibition at 0.01 mM
(1E)-1-[3,5-bis(methoxymethoxy)phenyl]-4,4-dimethylpent-1-en-3-one
14.9% inhibition at 0.01 mM
(1E,4E)-1,5-bis(4-hydroxy-3-methoxyphenyl)penta-1,4-dien-3-one
51.8% inhibition at 0.01 mM
(1E,4E)-1,5-bis[3,4-bis(methoxymethoxy)phenyl]penta-1,4-dien-3-one
84.3% inhibition at 0.01 mM
(1E,4E)-1-(2H-1,3-benzodioxol-5-yl)-5-[3,5-bis(methoxymethoxy)phenyl]penta-1,4-dien-3-one
57.4% inhibition at 0.01 mM
(1E,4E)-1-(4-hydroxy-3,5-dimethoxyphenyl)-5-(3,4,5-trimethoxyphenyl)penta-1,4-dien-3-one
82.9% inhibition at 0.01 mM
(1Z,4E)-1,5-bis[3,5-bis(methoxymethoxy)phenyl]-2-chloropenta-1,4-dien-3-one
83.2% inhibition at 0.01 mM
(1Z,4E)-5-[3,5-bis(methoxymethoxy)phenyl]-2-bromo-1-[2-bromo-3,5-bis(methoxymethoxy)phenyl]penta-1,4-dien-3-one
77.4% inhibition at 0.01 mM
(2aR,6aR,12bS,14bS)-10,17-dimethoxy-3,3,6,6-tetramethyl-2a,3,6a,7,12b,14b-hexahydro-2H,6H-chromeno[3,4-c]chromeno[4',3':4,5]pyrano[3,2-h]chromene-13,14-dione
-
inhibits Pgp- and MDR1-mediated daunorubicin transport in NIH-3T3 MDR1 cells
(2aR,6aS,12bR,14bS)-10,17-dimethoxy-3,3,6,6-tetramethyl-2a,3,6a,7,12b,14b-hexahydro-2H,6H-chromeno[3,4-c]chromeno[4',3':4,5]pyrano[3,2-h]chromene-13,14-dione
-
inhibits Pgp- and MDR1-mediated daunorubicin transport in NIH-3T3 MDR1 cells
(2E)-3-[3,5-bis(methoxymethoxy)phenyl]-N-methylprop-2-enamide
6.1% inhibition at 0.01 mM
(2E)-3-[3,5-bis(methoxymethoxy)phenyl]prop-2-enal
9.2% inhibition at 0.01 mM
(2E)-3-[3,5-bis(methoxymethoxy)phenyl]prop-2-enoic acid
0.3% inhibition at 0.01 mM
(2E,4E)-8-methyl-2,4-bis[(pyridin-3-yl)methylidene]-8-azabicyclo[3.2.1]octan-3-one
-
-
(2E,4E)-8-methyl-2,4-bis[(pyridin-4-yl)methylidene]-8-azabicyclo[3.2.1]octan-3-one
-
-
(2E,5E)-2,5-bis[(pyridin-3-yl)methylidene]cyclopentan-1-one
-
-
(2E,6E)-2,6-bis[(1-methyl-1H-imidazol-2-yl)methylidene]cyclohexan-1-one
-
-
(2E,6E)-2,6-bis[(1-methyl-1H-imidazol-5-yl)methylidene]cyclohexan-1-one
-
-
(2E,6E)-2,6-bis[(1-methyl-1H-indol-2-yl)methylidene]cyclohexan-1-one
-
-
(2E,6E)-2,6-bis[(1-methyl-1H-pyrrol-2-yl)methylidene]cyclohexan-1-one
-
-
(2E,6E)-2,6-bis[(2,5-dimethoxyphenyl)methylidene]cyclohexan-1-one
-
-
(2E,6E)-2,6-bis[(2-fluoro-4,5-dimethoxyphenyl)methylidene]cyclohexan-1-one
-
-
(2E,6E)-2,6-bis[(2-fluorophenyl)methylidene]cyclohexan-1-one
30.5% inhibition at 0.01 mM
(2E,6E)-2,6-bis[(2-fluoropyridin-3-yl)methylidene]cyclohexan-1-one
-
-
(2E,6E)-2,6-bis[(2-fluoropyridin-4-yl)methylidene]cyclohexan-1-one
-
-
(2E,6E)-2,6-bis[(3,4,5-trimethoxyphenyl)methylidene]cyclohexan-1-one
-
-
(2E,6E)-2,6-bis[(4-hydroxy-3-methoxyphenyl)methylidene]cyclohexan-1-one
-
-
(2E,6E)-2,6-bis[(pyridin-3-yl)methylidene]cyclohexan-1-one
-
-
(2E,6E)-2,6-bis[(pyridin-4-yl)methylidene]cyclohexan-1-one
-
-
(2E,6E)-2,6-bis[(thiophen-2-yl)methylidene]cyclohexan-1-one
-
-
(2E,6E)-2,6-bis[[3,5-bis(methoxymethoxy)phenyl]methylidene]cyclohexan-1-one
69.8% inhibition at 0.01 mM
(2R,4aR,7bR,9R,11aR,14bR)-2,5,5,9,12,12-hexamethyl-1,3,4,4a,5,8,9,10,11,11a,12,14b-dodecahydrobenzo[c]isochromeno[3,4-g]chromene-7,14(2H,7bH)-dione
-
inhibits Pgp- and MDR1-mediated daunorubicin transport in NIH-3T3 MDR1 cells
(3E,5E)-1-methyl-3,5-bis[(1-methyl-1H-imidazol-2-yl)methylidene]piperidin-4-one
-
-
(3E,5E)-1-methyl-3,5-bis[(3,4,5-trimethoxyphenyl)methylidene]piperidin-4-one
-
-
(3E,5E)-1-methyl-3,5-bis[(pyridin-3-yl)methylidene]piperidin-4-one
-
-
(3E,5E)-1-methyl-3,5-bis[(pyridin-4-yl)methylidene]piperidin-4-one
-
-
-
(3E,5E)-1-methyl-3,5-bis[(thiophen-2-yl)methylidene]piperidin-4-one
-
-
(3E,5E)-3,5-bis[(2,5-dimethoxyphenyl)methylidene]-1-methylpiperidin-4-one
-
-
(3E,5E)-3,5-bis[(2-fluoro-4,5-dimethoxyphenyl)methylidene]-1-methylpiperidin-4-one
-
-
(3E,5E)-3,5-bis[[3,5-bis(methoxymethoxy)phenyl]methylidene]-1-methylpiperidin-4-one
52% inhibition at 0.01 mM
(4E)-5-[3,5-bis(methoxymethoxy)phenyl]-2-[[3,4-bis(methoxymethoxy)phenyl]methyl]-3-oxopent-4-enenitrile
29.9% inhibition at 0.01 mM
(6aS,9bR,15aS,18bR)-2,4,11,13-tetrabromo-7,7,16,16-tetramethyl-6a,15a,16,18b-tetrahydro-6H,15H-chromeno[3,4-c]chromeno[4',3':4,5]pyrano[2,3-g]chromene-9,18(7H,9bH)-dione
-
inhibits Pgp- and MDR1-mediated daunorubicin transport in NIH-3T3 MDR1 cells
(6aS,9bR,15aS,18bR)-3,12-dimethoxy-7,7,16,16-tetramethyl-6a,15a,16,18b-tetrahydro-6H,15H-chromeno[3,4-c]chromeno[4',3':4,5]pyrano[2,3-g]chromene-9,18(7H,9bH)-dione
-
inhibits Pgp- and MDR1-mediated daunorubicin transport in NIH-3T3 MDR1 cells
(R)-4-[(1a,6,10b)-1,1-dichloro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl]-[(5-quinolinyloxy)methyl]-1-piperazineethanol
-
complete inhibition of P-glycoprotein at 0.005 mM
(R)-4-[(1a,6,10b)-1,1-difluoro-1,1a,6,10btetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl]-[(5-quin-olinyloxy)methyl]-1-piperazineethanol
-
LSN 335979, P-glycoprotein-specific inhibitor
1,13-bis[4'-(4H-chromen-4-on-2-yl)phenyl]-N-(benzyl)-1,4,10,13-tetraoxa-7-azatridecane
-
competitive inhibitor to doxorubicin binding by P-glycoprotein
1,5-bis[3,4-bis(methoxymethoxy)phenyl]-1,5-bis(phenylsulfanyl)pentan-3-one
26.6% inhibition at 0.01 mM
1,5-bis[3,4-bis(methoxymethoxy)phenyl]-1,5-bis[(2,3-dihydroxypropyl)sulfanyl]pentan-3-one
1.6% inhibition at 0.01 mM
1,5-bis[3,5-bis(methoxymethoxy)phenyl]-1,5-bis(ethylsulfanyl)pentan-3-one
37.1% inhibition at 0.01 mM
1-(4-acetylpiperazin-1-yl)-4-propoxy-9H-thioxanthen-9-one
-
uncompetitive, approximately 1.5fold more potent than verapamil in decreasing the doxorubicin GI50 on K-562 Dox cell line
1-isatin-4-(40-methoxyphenyl)-3-thiosemicarbazone
-
IC50 against KB-3-1 cells 0.0142 mM, against KB-VI cells 0.0033 mM. Displays MDR1-selectivity against all P-glycoprotein expressing cell lines examined, and cross-resistance is no observed. Selectivity is reversed by inhibitors of P-glycoprotein ATPase activity. Compound also shows selectivity for cells expressing mouse and hamster MDR1
1-isatin-4-(40-nitrophenyl)-3-thiosemicarbazone
-
IC50 against KB-3-1 cells 0.0171 mM, against KB-VI cells 0.0021 mM
1-isatin-4-(40-tert-butyl phenyl)-3-thiosemicarbazone
-
IC50 against KB-3-1 cells 0.0159 mM, against KB-VI cells 0.0148 mM
1-[[2-(4-nitrophenyl)ethyl]amino]-4-propoxy-9H-thioxanthen-9-one
-
uncompetitive, approximately 1.5fold more potent than verapamil in decreasing the doxorubicin GI50 on K-562 Dox cell line
10-(3-(dimethylamino)propyl)-2-(trifluoromethyl)phenothiazine
-
-
16alpha-17beta-estradiol 17-(beta-D-glucuronide)
-
transport of aflatoxin B1-epoxide-GSH conjugate
17-beta-estradiol 17-beta-(D-glucuronide)
17beta-estradiol 16-(beta-D-glucuronide)
-
transport of aflatoxin B1-epoxide-GSH conjugate
17beta-estradiol 3-sulfato-17-(beta-D-glucuronide)
-
transport of aflatoxin B1-epoxide-GSH conjugate
2'-(4-ethoxyphenyl)-5-(4-methylpiperazin-1-yl)-1H,1'H-2,5'-bibenzo[d]imidazole
-
almost complete inhibition of fish P-glycoprotein specific ATPase in micromolar concentrations
2,6-bis(4-(dimethylamino)phenyl)-4-(5-(piperidine-1-carbonothioyl)thien-2-yl)thiopyrylium chloride
-
81% inhibition of MRP1 at 0.01 mM
2,6-bis(4-(dimethylamino)phenyl)-4-(5-(piperidine-1-carbonyl)thien-2-yl)thiopyrylium hexafluorophosphate
-
78% inhibition of MRP1 at 0.01 mM
2,6-di-tert-butyl-4-(5-(piperidine-1-carbonothioyl)thien-2-yl)thiopyrylium hexafluorophosphate
-
11% inhibition of MRP1 at 0.01 mM
2,6-di-tert-butyl-4-(5-(piperidine-1-carbonothioyl)thiophen-2-yl)thiopyrylium chloride
-
32% inhibition of MRP1 at 0.01 mM
2-(4-maleimidoanilino)-naphthalene-6-sulfonic acid
-
-
2-tert-butyl-6-(4-(dimethylamino)phenyl)-4-(5-(piperidine-1-carbonothioyl)thiophen-2-yl)thiopyrylium chloride
-
93% inhibition of MRP1 at 0.01 mM
2-tert-butyl-6-(4-(dimethylamino)phenyl)-4-(5-(piperidine-1-carbonyl)thien-2-yl)thiopyrylium hexafluorophosphate
-
59% inhibition of MRP1 at 0.01 mM
2-[4-(3-ethoxy-1-propenyl)phenyl]-4,5-bis-[4-(2-propylamino)phenyl]-1H-imidazole
-
i.e. OC144-093. Coadministration of OC144-093 with docetaxel enhances the oral bioavailability of docetaxel to a limited extent (8-26%) in humans, and has a good safety profile as well
3,6-bis(dimethylamino)-9-(4-dimethylaminophenyl)-thioxanthylium hexafluorophosphate
-
competitive inhibition of verapamil-dependent ATPase-activity
3,6-bis(dimethylamino)-9-phenyl-selenoxanthylium bromide
-
i.e. selenium-derivative of tetramethylrosamine, competitive inhibition of verapamil-dependent ATPase-activity
3-[(3-[[(1,3-dioxo-8-phenyl-3,3a,3b,8,8a,8b-hexahydroindeno[1',2':3,4]cyclobuta[1,2-c]pyrrol-2(1H)-yl)acetyl]oxy]propyl)(methyl)amino]propyl (2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoate
-
-
3-[(3-[[(2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]oxy]propyl)amino]propyl (2E)-3-(anthracen-9-yl)prop-2-enoate
-
-
3-[(3-[[(2E)-3-(3,4-dimethoxyphenyl)prop-2-enoyl]oxy]propyl)(methyl)amino]propyl 10-chloroanthracene-9-carboxylate
-
-
3-[(3-[[(2E)-3-(3,4-dimethoxyphenyl)prop-2-enoyl]oxy]propyl)(methyl)amino]propyl 3,4,5-trimethoxybenzoate
-
-
3-[(3-[[(2E)-3-(3,4-dimethoxyphenyl)prop-2-enoyl]oxy]propyl)(methyl)amino]propyl anthracene-9-carboxylate
-
-
3-[(3-[[3-(1,3-dioxo-8-phenyl-3,3a,3b,8,8a,8b-hexahydroindeno[1',2':3,4]cyclobuta[1,2-c]pyrrol-2(1H)-yl)propanoyl]oxy]propyl)(methyl)amino]propyl (2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoate
-
-
3-[(3-[[3-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)propanoyl]oxy]propyl)(methyl)amino]propyl (2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoate
-
-
3-[(3-[[bis(4-methoxyphenyl)acetyl]oxy]propyl)(methyl)amino]propyl (2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoate
-
-
3-[methyl(3-[[(2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]oxy]propyl)amino]propyl (2E)-3-(3,4-dimethoxyphenyl)prop-2-enoate
-
-
3-[methyl(3-[[(2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]oxy]propyl)amino]propyl (2E)-3-(anthracen-9-yl)prop-2-enoate
-
-
3-[methyl(3-[[(2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]oxy]propyl)amino]propyl (2E)-3-(biphenyl-4-yl)prop-2-enoate
-
-
3-[methyl(3-[[(2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]oxy]propyl)amino]propyl 3,3-diphenylprop-2-enoate
-
-
3-[methyl(3-[[(2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]oxy]propyl)amino]propyl 3,4,5-trimethoxybenzoate
-
-
3-[methyl(3-[[(2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]oxy]propyl)amino]propyl anthracene-9-carboxylate
-
-
3-[methyl(3-[[(2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]oxy]propyl)amino]propyl biphenyl-4-carboxylate
-
-
3-[[3-[(diphenylacetyl)oxy]propyl](methyl)amino]propyl (2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoate
-
-
4-(2-aminoethyl)benzenesulfonylfluoride
-
-
4-[5-(4-chlorophenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide
-
i.e. SC236. The direct inhibitory effects of indomethacin and SC236 on P-gp may contribute to their ability to increase the intracellular retention of doxorubicin and thus enhance its cytotoxicity
5'-O-[4-(fluorosulfonyl)benzoyl]adenosine
-
incubation inhibits ATP hydrolysis and the binding of 8-azido-ATP. 5'-Fluorosulfonylbenzoyl 5'-adenosine is an ATP analog that interacts with both the drug-binding and ATP-binding sites of P-gp, but fluorosulfonyl-mediated crosslinking is observed only at the nucleotide-binding domains
5-[(5-[[(2E)-3-(3,4-dimethoxyphenyl)prop-2-enoyl]oxy]pentyl)(methyl)amino]pentyl 3,4,5-trimethoxybenzoate
-
-
5-[(5-[[(2E)-3-(3,4-dimethoxyphenyl)prop-2-enoyl]oxy]pentyl)(methyl)amino]pentyl anthracene-9-carboxylate
-
-
5-[(5-[[bis(4-methoxyphenyl)acetyl]oxy]pentyl)(methyl)amino]pentyl (2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoate
-
-
5-[methyl(5-[[(2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]oxy]pentyl)amino]pentyl (2E)-3-(biphenyl-4-yl)prop-2-enoate
-
-
5-[methyl(5-[[(2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]oxy]pentyl)amino]pentyl 3,3-diphenylprop-2-enoate
-
-
6-[(2S,4R,6E)-4-methyl-2-(methylamino)-3-oxo-6-octenoic acid]cyclosporine D
-
-
9,10-dihydro-5-methoxy-9-oxo-N-{4-[2-(1,2,3,4-tetrahydro-6,7-dimethoxy-2-isoquinolinyl)ethyl]phenyl}-4-acridine
-
i.e. GF120918. A good and safe P-gp inhibitor alternative for cyclosporin A in enhancing the oral bioavailability of paclitaxel
actinomycin D
-
inhibits transport of Hoechst 3343 and rhodamine 123
alpha-mangostin
effectively and selectively inhibits enzyme-mediated drug transport and reverses multidrug resistance in ABCG2-overexpressing cancer cells
ATPgammaS
-
existence of two binding sites for ATPS with remarkably different binding affinities. One site binds ATPgammaS with Kd of 6 microM and the second binds ATPgammaS with Kd of 0.74 mM
auraptene
-
stimulates the ATPase activity of MRP1. No inhibition of MRP1-mediated efflux by auraptene, but auraptene increases the accumulation of daunorubicin in KB-C2 cells
azido-ATP
-
competitive, binding activity of wild-type and mutant enzymes, overview
azidophenacylglutathione
-
competitive inhibitor of daunorubicin transport
Ba2+
-
1 mM, 90% loss of activity
beta,gamma-methylene adenosine 5'-triphosphate
-
-
beta-sitosterol-O-glucoside
-
inhibits the efflux of the P-gp substrate rhodamine 123 in a concentration-dependent manner. Good candidates for the development of novel P-gp/MDR1 reversal agents which may enhance the accumulation and efficacy of chemotherapy agents
bis[(4aS,6R,8aS)-3-methoxy-11-methyl-5,6,9,10,11,12-hexahydro-4aH-[1]benzofuro[3a,3,2-ef][2]benzazepin-6-yl] decanedioate
-
galactamine dimer. the inhibitory activity of the inhibitor on P-gp transport of substrate is evaluated in cells that over-express P-gp
buprenorphine
-
inhibits paclitaxel transport, placental brush border membrane vesicles
byakangelicol
-
shows strong P-gp inhibition from the screening of P-gp inhibitor evaluated by quinidine permeation through the Caco-2 monolayer
carnosic acid
-
increases the accumulation of daunorubicin or rhodamine 123 in KB-C2 cells. The ATPase activity of P-glycoprotein is stimulated
carnosol
-
increases the accumulation of daunorubicin or rhodamine 123 in KB-C2 cells. The ATPase activity of P-glycoprotein is stimulated
cis-(Z)-flupentixol
-
is a non-competitive inhibitor that interacts with the substrate site but is not transported
D-alpha-tocopheryl polyethylene glycol 1000 succinate
-
i.e. TPGS 1000, water-soluble Vitamin E derivative. Inhibits substrate-induced ATPase activity without inducing significant ATPase activity on its own. Modulation of ATPase activity correlates with inhibitory potential for P-glycoprotein-mediated efflux
-
daunorubicin
-
inhibits transport of rhodamine 123
deacetylnomilin
-
inhibits the efflux of the P-gp substrate rhodamine 123 in a concentration-dependent manner. Good candidates for the development of novel P-gp/MDR1 reversal agents which may enhance the accumulation and efficacy of chemotherapy agents. Good candidates for the development of novel P-gp/MDR1 reversal agents which may enhance the accumulation and efficacy of chemotherapy agents
desloratadine
-
weakly inhibits daunorubicin transport, 19% of the inhibition caused by vanadate, IC50: 0.043 nM, desloratadine is no significant inhibitor of P-gp and should not cause clinical drug interactions with agents that are P-gp substrates
diclofenac
-
inhibits MRP2-mediated drug transport
Digitonin
-
inhibits ATPase activity of P-gp
dodecyloctaglycol
-
uncompetitive inhibition of verapamil-induced Pgp ATPase activity
estradiol 17beta-D-glucuronide
-
competitive inhibition of the transport activity of Mdr2
etoposide
-
inhibits transport of Hoechst 3343 and rhodamine 123
flavonoids
-
useful inhibitors for clinical application to multidrug resistance
flurazepam
-
inhibits daunorubicin efflux up to 80%, partially inhibits ATPase activity
gomisin A
-
strongly inhibits P-glycoprotein ATPase activity in cells overexpressing the enzyme. Alters substrate interaction of P-glycoprotein but itself is neither a substrate nor a competitive inhibitor
HEPES
-
uptake of P-glycoprotein substrates is substantially diminished when the HEPES concentration is raised to 25 mM. Addition of 15 or 25 mM HEPES in the uptake buffer results in significant reduction in the accumulation of P-glycoprotein substrates cyclosporine-A, ritonavir, and lopinavir. Bidirectional A-B and B-A transport studies show that permeability ratio in the presence of 25 mM HEPES is significantly higher than control. HEPES stimulates the production of ATP and modulates the energy dependent efflux and uptake processes
hesperidin
-
inhibits the efflux of the P-gp substrate rhodamine 123 in a concentration-dependent manner. Good candidates for the development of novel P-gp/MDR1 reversal agents which may enhance the accumulation and efficacy of chemotherapy agents
Hoechst 33342
inhibition of doxorubicin transport by Hoechst 33342 occurs by a competitive mechanism
limonin
-
inhibits the efflux of the P-gp substrate rhodamine 123 in a concentration-dependent manner. Good candidates for the development of novel P-gp/MDR1 reversal agents which may enhance the accumulation and efficacy of chemotherapy agents
loratadine
-
inhibits daunorubicin transport, IC50: 0.011 nM, much less inhibitory than cyclosporin A or verapamil, 43% of the inhibition caused by vanadate
lovastatin
-
increases the absorption of verapamil (used as an antiarrhythmic agent to control supraventricular tachyarrhythmias) by inhibiting P-glycoprotein
methadone
-
inhibits paclitaxel transport, placental brush border membrane vesicles
methoxypolyethylene17 glycol-beta-caprolactone5
-
amphiphilic diblock copolymer, decreases membrane fluidity and inhibits enzyme-mediated efflux while stimulating the enzyme's ATPase activity up to 3fold
methyl (2E)-3-[3,5-bis(methoxymethoxy)phenyl]prop-2-enoate
8.6% inhibition at 0.01 mM
methylparathion
-
0.05 mM, stimulates ATPase activity by 30% and inhibits at higher concentrations
N,N'-[[1,5-bis[3,4-bis(methoxymethoxy)phenyl]-3-oxopentane-1,5-diyl]bis(sulfanediylethane-2,1-diyl)]diacetamide
15.2% inhibition at 0.01 mM
N-(2'-deoxy-beta-D-ribofuranosyl)-5-cyclohexyl-1H-indole
-
nontransported substrate of P-glycoprotein
N-(4-[2-(1,2,3,4-tetrahydro-6,7-dimethoxy-2-isoquinolinyl)ethyl]-phenyl)-9,10-dihydro-5-methoxy-9-oxo-4-acridine carboxamide
-
-
N-methyl-N-(9-phenyl-2,3,6,7-tetrahydro-1H,5H,12H-pyrido[3,2,1-ij]selenochromeno[2,3-f]quinolin-12-ylidene)methanaminium hexafluorophosphate
N-methyl-N-(9-phenyl-2,3,6,7-tetrahydro-1H,5H,12H-pyrido[3,2,1-ij]thiochromeno[2,3-f]quinolin-12-ylidene)methanaminium hexafluorophosphate
-
competitive inhibition of verapamil-dependent ATPase-activity
N-[5-[1-(4-[2-[6-methoxy-7-[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]-3,4-dihydroisoquinolin-2(1H)-yl]ethyl]phenyl)-1H-1,2,3-triazol-4-yl]-2-propanoylphenyl]quinoline-2-carboxamide
-
N-[6-(dimethylamino)-9-[5-(piperidin-1-ylcarbonyl)thiophen-2-yl]-3H-selenoxanthen-3-ylidene]-N-methylmethanaminium hexafluorophosphate
-
-
N-[6-(dimethylamino)-9-[5-(piperidin-1-ylcarbonyl)thiophen-2-yl]-3H-telluroxanthen-3-ylidene]-N-methylmethanaminium hexafluorophosphate
-
-
N-[6-(dimethylamino)-9-[5-(piperidin-1-ylcarbonyl)thiophen-2-yl]-3H-thioxanthen-3-ylidene]-N-methylmethanaminium hexafluorophosphate
-
-
N-[9-[3-(dimethylamino)phenyl]-2,3,6,7-tetrahydro-1H,5H,12H-pyrido[3,2,1-ij]selenochromeno[2,3-f]quinolin-12-ylidene]-N-methylmethanaminium bromide
-
-
N-[9-[4-(dimethylamino)phenyl]-2,3,6,7-tetrahydro-1H,5H,12H-pyrido[3,2,1-ij]selenochromeno[2,3-f]quinolin-12-ylidene]-N-methylmethanaminium bromide
-
-
nanoparticles
-
doxorubicin and paclitaxel nanoparticles inhibit P-glycoprotein and transiently deplete ATP, while cyclosporine A and polystyrene nanoparticles do not, overview
-
naringin
-
i.e. 7-[[2-O-(6-deoxy-alpha-L-mannopyra nosyl)-beta-D-glucopyranosyl]oxy]-2,3-dihydro-5-hydroxy-2-(4-hydroxyphenyl)-4H-1-benzo pyran-4-one. Pre-treatment with naringin prior to doxorubicin treatment increases the sensitivity of the enzyme to doxorubicin, naringin inhibits the doxorubicin-stimulated ATPase activity and may interact directly with the transporter. Naringin seems to modulate the in vivo expression of P-gp
neohesperidin
-
inhibits the efflux of the P-gp substrate rhodamine 123 in a concentration-dependent manner. Good candidates for the development of novel P-gp/MDR1 reversal agents which may enhance the accumulation and efficacy of chemotherapy agents
nobiletin
-
a chemopreventive citrus phytochemical from orange, stimulates the ATPase activity of MRP1. Nobiletin also increases the accumulation of calcein, a fluorescent substrate of MRP1, in KB/MRP cells, and of P-glycoprotein substrate daunorubicin in KB-C2 cells
Pb2+
-
3 mM, 77% loss of activity
poly(acrylic acid)cysteine
-
praeruptorin A
-
modulates Pgp expression
procyanidin
-
markedly increases the accumulation of rhodamine 123 by inhibiting its efflux in a dose-dependent manner. A 5-fold increase in cellular Rh123 is observed for procyanidine at 0.01 mM. Procyanidine is a potent inhibitor of P-glycoprotein on blood-brain barrier and can improve the therapeutic effects on cerebral tumors of some drugs which are difficult to accumulate in the brain
PSC 833
-
PgP inhibitors increase uptake of doxorubicin in tumor cells close to blood vessels, have little effect on drug uptake into tumor cells at intermediate distances, and might have a paradoxical effect to decrease doxorubicin uptake into distal tumor cells. This effect probably contributes to the limited success of PgP inhibitors in clinical trials
RC21v3
-
potent inhibitor
resveratrol disulfate
-
acts as a competitive inhibitor of BCRP-mediated methotrexate transport
rifampicin
inhibition of doxorubicin transport by rifampicin occurs by a competitive mechanism
rivulobirin A
-
shows strong P-gp inhibition from the screening of P-gp inhibitor evaluated by quinidine permeation through the Caco-2 monolayer
S-(2,4-dinitrophenyl)glutathione
-
competitive
S-(p-azidophenylacyl)-glutathione
-
competitive
S-butyl glutathione
-
transport of aflatoxin B1-epoxide-GSH conjugate
S-hexyl glutathione
-
transport of aflatoxin B1-epoxide-GSH conjugate
S-octyl glutathione
-
transport of aflatoxin B1-epoxide-GSH conjugate
S-propyl (2E)-3-[3,5-bis(methoxymethoxy)phenyl]prop-2-enethioate
28.2% inhibition at 0.01 mM
salinomycin
-
treatment of the multidrug resistant cell lines with salinomycin restores a normal drug sensitivity of these cells
semi-beta-carotene-epoxide
-
-
sildenafil
-
potent inhibition of MRP4
Sodium vanadate
-
0.01 mM, 90% loss of activity
stigmasterol
-
inhibits the efflux of the P-gp substrate rhodamine 123 in a concentration-dependent manner. Good candidates for the development of novel P-gp/MDR1 reversal agents which may enhance the accumulation and efficacy of chemotherapy agents
taurochenodeoxycholic acid
-
tert-butyl (3E,5E)-3,5-bis[(2,5-dimethoxyphenyl)methylidene]-4-oxopiperidine-1-carboxylate
-
-
tert-butyl (4R)-4-(benzyloxy)-1-(tert-butoxycarbonyl)-L-prolyl-N6-[(benzyloxy)carbonyl]-L-lysinate
tert-butyl 3-[(3S,6S,12aS)-6-(2-methylpropyl)-1,4-dioxo-9-[(prop-2-en-1-yl)oxy]-1,2,3,4,6,7,12,12a-octahydropyrazino[1',2':1,6]pyrido[3,4-b]indol-3-yl]propanoate
-
tert-butyl 3-[(3S,6S,12aS)-9-(cyclopentyloxy)-6-(2-methylpropyl)-1,4-dioxo-1,2,3,4,6,7,12,12a-octahydropyrazino[1',2':1,6]pyrido[3,4-b]indol-3-yl]propanoate
-
tert-butyl [(3S,6S,12aS)-9-methoxy-6-(2-methylpropyl)-1,4-dioxo-1,2,3,4,6,7,12,12a-octahydropyrazino[1',2':1,6]pyrido[3,4-b]indol-3-yl]acetate
-
tert-butyl [4-[(3S,6S,12aS)-9-methoxy-6-(2-methylpropyl)-1,4-dioxo-1,2,3,4,6,7,12,12a-octahydropyrazino[1',2':1,6]pyrido[3,4-b]indol-3-yl]butyl]carbamate
-
tetrahydrocurcumin
-
inhibitory to P-glycoprotein as well as to mitoxantrone resistance protein and multidrug resistance protein1. Inhibition of transport function with concomitant stimulation of ATPase activity
tetraphenylphosphonium
-
-
trans,trans-4,17(20)-pregnadiene-3,16-dione
-
i.e. Z-guggulsterone. In presence of guggulsterone, fluorescent substrates daunorubicin or rhodamine 123 accumulate in KB-C2 cells. Efflux of rhodamine 123 is inhibited and the accumulation of substrate calcein is increased. ATPase activities of both isoforms ABCB1 And ABCC1 are stimulated
Triton X-100
-
uncompetitive inhibition of verapamil-induced Pgp ATPase activity
Tween 80
-
uncompetitive inhibition of verapamil-induced Pgp ATPase activity
ursolic acid
-
increases the accumulation of daunorubicin or rhodamine 123 in KB-C2 cells. The ATPase activity of P-glycoprotein is stimulated
vincristine
-
alone is a very poor inhibitor of transport of leukotriene C4, together with GSH acts as relatively potent competitive inhibitor
wogonin
-
impairs the function of P-glycoprotein and increases cellular content of etoposide in HL-60 cells. Wogonin may be used to reduce the excretion of anticancer agents via P-glycoprotein and to increase the pharmacological action in cancer cells. Wogonin may play a role in overcoming multidrug resistance
XR9576
-
is a non-competitive inhibitor that interacts with the substrate site but is not transported
[2-(1H-benzimidazol-2-yl)ethanamine]-4-propoxy-9H-thioxanthen-9-one
-
uncompetitive, causes an accumulation rate of rhodamine-123 similar to that caused by verapamil in the K-562 Dox resistant cell line, and a decrease in ATP consumption by P-gp. At 10 mM, 12.5fold decrease in the GI50 value of doxorubicin in the K-562 Dox resistant cell line, being 2fold more potent than verapamil
17-beta-estradiol 17-beta-(D-glucuronide)
-
-
17-beta-estradiol 17-beta-(D-glucuronide)
-
transport of aflatoxin B1-epoxide-GSH conjugate
ADP
-
-
arsenate
-
competitive inhibitor of daunorubicin transport
benzbromarone
-
-
benzbromarone
-
50% inhibition of N-ethylmaleimide S-glutathione activated ATPase activity of MRP1 at 0.01 mM, 50% inhibition of E217betaG uptake by MRP1 at 0.005-0.008 mM, inhibits E217betaG uptake by MRP3 at 0.05 mM, but greatly stimulates this activity at 0.001-0.02 mM
beryllium fluoride
-
0.25 mM, 86% inhibition of ATPase, 89% inhibition of UTPase, and 50% inhibition of GTPase activity
cholesterol
-
presence of cholesterol in the bilayer modulates the basal and drug-stimulated ATPase activity of reconstituted Pgp in vesicles. Both the ability of drugs to bind to the protein and the drug transport and phospholipid flippase functions of Pgp are also affected by cholesterol. The effects of cholesterol on drug binding affinity are unrelated to the size of the compound. Increasing cholesterol content greatly alters the partitioning of hydrophobic drug substrates into the membrane, which may account for some of the effects of cholesterol on Pgp-mediated drug transport
cholesterol
-
presence of cholesterol in liposomes increases the binding affinity of small drug substrates with molecular masses below 500 Da, does not affect that of drugs with molecular mass of between 800 and 900 Da, and suppresses that of valinomycin with a molecular mass greater than 1000
clotrimazole
-
noncompetitive, inhibitor interacts with the transporter at a site distinct from the ATP-binding domains. Transport of clotrimazole by the enzyme continues at intracellular concentrations of clotrimazole that should eliminate all ATPase activity. GTPase and UTPase activites of the enzyme are rather resistant to clotrimazole
Colchicine
-
inhibits transport of Hoechst 3342
curcumin
-
-
curcumin
-
modulates Pgp expression
curcumin
99.5% inhibition at 0.01 mM
cyclosporin A
-
inhibits the transport of tetramethylrosamine in a concentration-dependent manner, 0.004 mM: almost complete inhibition, competes for tetramethylrosamine transport at the drug binding site
cyclosporin A
-
weak competitive inhibitor of daunorubicin transport
cyclosporin A
-
inhibits daunorubicin transport, IC50: 0.001 nM
cyclosporin A
-
inhibits CD4 T cell P-glycoprotein activity in HIV-infected adults initiating treatment with nucleoside reverse transcriptase inhibitors
cyclosporin A
-
uncompetitive inhibition of the detergentinduced activity
cyclosporin A
-
inhibits transport of dexamethasone, ritonavir and vinblastine
cyclosporine A
-
-
cyclosporine A
-
almost complete inhibition of fish P-glycoprotein specific ATPase in nanomolar concentrations
dipyridamole
-
potent inhibition of MRP4
doxorubicin
-
inhibits transport of rhodamine 123
doxorubicin
-
cis-inhibition without trans-inhibition on MDR1-mediated vinblastine efflux of Xenopus laevis oocytes expressing human P-glycoprotein
EDTA
-
partial
elacridar
-
inhibits P-gp
genistein
-
competitive inhibitor of daunorubicin transport
glibenclamide
-
mutation of residue Tyr2 in MRP1 cannot alter the sensitivity to glibenclamide
glyceollins
-
-
GSH
-
alone is a very poor inhibitor of transport of leukotriene C4, together with vincristine acts as relatively potent competitive inhibitor
GSH
-
competitive inhibitor of daunorubicin transport
GSSG
-
-
GSSG
-
transport of aflatoxin B1-epoxide-GSH conjugate
GSSG
-
competitive inhibitor of daunorubicin transport
indomethacin
-
-
indomethacin
-
an inhibitor of MRP1
indomethacin
-
the direct inhibitory effects of indomethacin and SC236 on P-gp may contribute to their ability to increase the intracellular retention of doxorubicin and thus enhance its cytotoxicity
Ko143
-
-
leukotriene D4
-
transport of aflatoxin B1-epoxide-GSH conjugate
leukotriene D4
-
competitive
methyl-beta-cyclodextrin
-
over 85% inhibition of ATPase at 10 mM, about 55% inhibition of the lipid flippase at 10 mM
methyl-beta-cyclodextrin
-
inhibits ATPase activity of P-gp, 5-10 mM, total inhibition
MK-571
-
-
MK-571
-
an inhibitor of MRP1
MK571
-
the leukotriene receptor antagonist
MK571
-
competitive inhibitor of daunorubicin transport
MK571
-
50% inhibition of N-ethylmaleimide S-glutathione activated ATPase activity of MRP1 at 0.01 mM, but slightly activates this activity at 500-2000 nM, 100% inhibition of E217betaG uptake by MRP1 at 0.01-0.05 mM, but stimulates this activity at 500-1000 nM, inhibits E217betaG uptake by MRP3 at 0.05-0.1 mM, but stimulates this activity at 0.002-0.005 mM
monoclonal antibiodies
-
monoclonal antibodies QCRL-2, QCRL-3, and QCRL-4 recognize distinct, non-overlapping epitopes of the enzyme MRP. The ability to inhibit MRP-dependent transport results from direct interactions with the nucleotide-binding domains of the protein that do not prevent the binding of ATP
-
monoclonal antibiodies
-
-
-
N-ethylmaleimide
-
0.1 mM, 70% loss of activity
N-ethylmaleimide
-
partial
N-methyl-N-(9-phenyl-2,3,6,7-tetrahydro-1H,5H,12H-pyrido[3,2,1-ij]selenochromeno[2,3-f]quinolin-12-ylidene)methanaminium hexafluorophosphate
-
-
N-methyl-N-(9-phenyl-2,3,6,7-tetrahydro-1H,5H,12H-pyrido[3,2,1-ij]selenochromeno[2,3-f]quinolin-12-ylidene)methanaminium hexafluorophosphate
-
competitive inhibition of verapamil-dependent ATPase-activity
oligomycin
-
-
oligomycin
-
inhibition of ATPase activity
ortho-vanadate
-
specific inhibitor
orthovanadate
-
rapid and complete inhibition in the presence of ATP and Co2+, very stable Pgp-ADP-Vi-Co2+ complex
orthovanadate
-
non-covalent inhibitor of ABC ATPases catalyzing a photo-oxidative cleavage, characterization of three cleavage sites within MRP1, influence of nucleotides and transported substrates on the cleavage reaction, mechanism
orthovanadate
-
0.3 mM, 93% inhibition of ATPase, 66% inhibition of UTPase, and 45% inhibition of GTPase activity
orthovanadate
-
complete inhibition at 4 mM
poly(acrylic acid)cysteine
-
-
poly(acrylic acid)cysteine
-
-
probenecid
-
-
probenecid
-
0.1 mM, 80% loss of activity
progesterone
-
inhibition of ATPase-activity arising from co-expression of isoforms ABCG5 and ABCG8
PSC833
-
weak competitive inhibitor of daunorubicin transport
PSC833
-
specific P-gp inhibitor
PSC833
-
potent inhibitor in nanomolar concentrations, with some residual activity
quercetin
-
inhibits transport of Hoechst 33342
quinidine
-
trans-inhibition on MDR1-mediated vinblastine and digoxin efflux of Xenopus laevis oocytes expressing human P-glycoprotein
quinidine
-
inhibits transport of dexamethasone, ritonavir and vinblastine
reserpine
-
rhodamine 6G
-
-
ritonavir
-
ritonavir
-
inhibition of intestinal P-glycoprotein by ritonavir causes increased darunavir absorption
S-decyl-glutathione
-
competitive
tariquidar
-
XR9576
tariquidar
the substrate inhibits P-gp ATPase activity in membranes, but stimulates ATPase activity when purified P-gp is assayed in the in the presence of n-dodecyl-beta-D-maltoside/sheep brain lipids. When wild-type human P-gp is expressed in Sf9 insect cells and the membranes are assayed for activity in the absence or presence of saturating concentrations of tariquidar, tariquidar reduces basal ATPase activity by about 60%
tert-butyl (4R)-4-(benzyloxy)-1-(tert-butoxycarbonyl)-L-prolyl-N6-[(benzyloxy)carbonyl]-L-lysinate
-
noncompetitive inhibitor towards daunorubicin and Hoechst 33342
tert-butyl (4R)-4-(benzyloxy)-1-(tert-butoxycarbonyl)-L-prolyl-N6-[(benzyloxy)carbonyl]-L-lysinate
-
noncompetitive inhibitor towards daunorubicin and Hoechst 33342
tetrandrine
-
i.e (1beta,1'beta)-6,6',7,12-tetramethoxy-2,2'-dimethylberbaman
tryptanthrin
-
vanadate
-
inhibits ATPase activity, 0.01 mM, 50% inhibition
vanadate
-
ATPase activity is highly sensitive to vanadate inhibition, 0.01 mM: 50% inhibition
vanadate
complete inhibition at 1 mM
vanadate
-
inhibits Pgp ATPase and tetramethylrosamine transport activity, interacts with the nucleotide-binding domain
vanadate
-
2 mM, 90% inhibition
vanadate
-
0.01 mM, the basal and fenvalerate or verapamil-stimulated ATPase activities are inhibited
vanadate
-
vanadate-sensitive ATPase activity
vanadate
-
very potent inhibitor of MDR1 efflux function
vanadate
-
inhibits ATPase activity
vanadate
-
vanadate-sensitive ATPase activity
vanadate
-
inhibits the ATPase activity of MRP2
vanadate
complete inhibition of doxorubicin transport at 0.1 mM vanadate
verapamil
-
inhibits the transport of tetramethylrosamine in a concentration-dependent manner, 0.02 mM: almost complete inhibition, competes for tetramethylrosamine transport at the drug binding site
verapamil
-
weak competitive inhibitor of daunorubicin transport
verapamil
-
inhibits daunorubicin transport, IC50: 0.004 nM
verapamil
-
inhibits efflux of rhodamine 123 uncompetitively
verapamil
-
the substrate is one of the most potent activators of P-gp ATPase activity, but inhibits calcein uptake
verapamil
-
trans-inhibition on MDR1-mediated vinblastine and digoxin efflux of Xenopus laevis oocytes expressing human P-glycoprotein
verapamil
-
inhibition of P-gp enhances the suppressive effect of kaempferol on aryl hydrocarbon receptor (AhR) transformation through an increase in the intracellular kaempferol concentration
verapamil
-
PgP inhibitors increase uptake of doxorubicin in tumor cells close to blood vessels, have little effect on drug uptake into tumor cells at intermediate distances, and might have a paradoxical effect to decrease doxorubicin uptake into distal tumor cells. This effect probably contributes to the limited success of PgP inhibitors in clinical trials
verapamil
-
inhibits transport of dexamethasone, ritonavir and vinblastine
verapamil
inhibits transport of doxorubicin by a non-competitive mechanism
vinblastine
-
higher concentrations of vinblastine prevent the transport of Hoechst 33342, but low concentrations stimulate the transport of Hoechst 33342
vinblastine
-
inhibits transport of Hoechst 3343 and rhodamine 123
zosuquidar
-
-
additional information
-
not inhibited by colchicine
-
additional information
-
the enzyme is inhibited by the transported substrates
-
additional information
-
SDS, Triton X-100, urea, EGTA, EDTA, DTT and 1,10-phenanthroline have no significant effect on activity
-
additional information
-
ATPase activity associated with P-glycoprotein is characterized by three drug-dependent phases: basal without drug, drug-activated, and drug-inhibited
-
additional information
-
no inhibition by buthionine sulfoximine
-
additional information
-
flavonoids inhibit the MRP1-mediated efflux of fluorescent substrate both from human erythrocytes and MDA-MB-231 resistant breast cancer cells, enzyme molecular modeling, overview
-
additional information
-
inhibition kinetics, overview
-
additional information
-
inhibitor effects on daunorubicin resistance and cell growth, overview
-
additional information
-
no effect by glutathione
-
additional information
-
the main mechanisms of P-gp inhibitors involves the regulation of P-gp expression by binding to drug binding sites or modulator binding sites
-
additional information
-
CACO-2 cell monolayer experiments preincubated with the nonionic surfactant TPGS 1000 (D-alpha-tocopheryl polyethylene glycol 1000 succinate), produce stronger substrate inhibitory activity than those conducted by direct substrate and surfactant coapplication. TPGS 1000 does not function as a competitive inhibitor in P-gp substrate efflux transport
-
additional information
-
no effect by glutathione
-
additional information
-
ethynylestradiol selectively diminishes the expression of Mdr2 in the intestine, no inhibition of expression of breast cancer resistance protein, of Mrp3, and expression of multidrug resistance protein 1 is only minimally impaired
-
additional information
not inhibited by rhodamine 123, rhodamine 6G, rhodamine B, quinine, and tetramethylrhodamine
-
additional information
-
not inhibited by rhodamine 123, rhodamine 6G, rhodamine B, quinine, and tetramethylrhodamine
-
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