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(3R,5R)-7-(1-ethyl-3-(4-fluorophenyl)-4-methyl-5-[(5-methyl-pyrazin-2-ylmethyl)-carbamoyl]-1H-pyrrol-2-yl)-3,5-dihydroxy-heptanoic acid sodium salt
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(3R,5R)-7-[1-ethyl-3-(4-fluorophenyl)-4-methyl-5-phenylcarbamoyl-1H-pyrrol-2-yl]-3,5-dihydroxy-heptanoicacid sodium salt
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(3R,5R)-7-[1-ethyl-3-(4-fluorophenyl)-5-(4-methoxybenzylcarbamoyl)-4-methyl-1H-pyrrol-2-yl]-3,5-dihydroxy-heptanoic acid sodium salt
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(3R,5R)-7-[1-ethyl-3-(4-fluorophenyl)-5-(4-methoxycarbonyl-benzylcarbamoyl)-4-methyl-1H-pyrrol-2-yl]-3,5-dihydroxy-heptanoic acid sodium salt
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(3R,5R)-7-[3-(4-fluoro-phenyl)-1-isopropyl-5-phenylcarbamoyl-4-pyridin-2-yl-1H-pyrrol-2-yl]-3,5-dihydroxy-heptanoic acid sodium salt
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(3R,5R)-7-[3-(4-fluorophenyl)-1-isopropyl-4-phenyl-5-phenylcarbamoyl-1H-pyrrol-2-yl]-3,5-dihydroxy-heptanoic acid sodium salt
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(3R,5R)-7-[3-(4-fluorophenyl)-5-[(3-methoxybenzyl)carbamoyl]-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
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(3R,5R)-7-[3-(4-fluorophenyl)-5-[[4-(methoxymethyl)benzyl]carbamoyl]-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
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(3R,5R)-7-[5-(4-carboxy-benzylcarbamoyl)-ethyl-3-(4-fluorophenyl)-4-methyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoicacid disodium salt
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(3R,5R)-7-[5-benzylcarbamoyl-3-(4-fluoro-phenyl)-1-isopropyl-4-pyridin-2-yl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoicacid
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(3R,5R)-7-[5-carbamoyl-1-ethyl-3-(4-fluorophenyl)-4-methyl-1H-pyrrol-2-yl]-3,5-dihydroxy-heptanoic acid sodium salt
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(3R,5R)-7-[5-carbamoyl-3-(4-fluoro-phenyl)-1-isopropyl-4-pyridin-2-yl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoicacid sodium salt
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(3R,5R)-7-[5-cyano-3-(4-fluoro-phenyl)-1-isopropyl-4-pyridin-2-yl-1H-pyrrol-2-yl]-3,5-dihydroxy-heptanoicacid sodium salt
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(3R,5R)-7-[5-[(3-carbamoylbenzyl)carbamoyl]-3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
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(3R,5R)-7-[5-[(4-cyanobenzyl)carbamoyl]-3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
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(3R,5R)-7-[5-[[4-(dimethylcarbamoyl)benzyl]carbamoyl]-3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
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(5S)-5-hydroxy-4-{2-[(1S,2R,4aR)-1,2,4a,5-tetramethyl-1,2,3,4,4a,7,8,8a-octahydronaphthalen-1-yl]ethyl}furan-2(5H)-one
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22.65% inhibition of HMG-CoA reductase at 0.001 mM concentration and maximum inhibition of 78.03% at 0.1 mM, the HMG-CoA reductase inhibitor, a clerodane diterpene from ethanolic extract of Polyalthia longifolia var. pendula, is a potential lipid lowering agent, molecular docking analysis, overview
(E,3R,5S)-7-(4-(3-(4-fluorophenyl)pentan-3-yl)-2-isopropylphenyl)-3,5-dihydroxyhept-6-enoic acid
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competitive inhibitor, shows slight inhibitory activity
(R)-3-hydroxy-3-methylglutaryl-CoA
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competitive inhibitor
(S)-4-carboxy-3-hydroxy-3-methylbutyryl-CoA
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competitive inhibitor
(S)-4-carboxy-3-hydroxybutyryl-CoA
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competitive inhibitor
3,3-dimethylglutaryl-CoA
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competitive inhibitor
3-hydroxy-3-methylglutaryl-CoA
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0.05 mM
3-hydroxyglutaryl-CoA
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competitive inhibitor
3-methylglutaryl-CoA
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competitive inhibitor
4-[[([5-[(3R,5R)-6-carboxy-3,5-dihydroxyhexyl]-4-(4-fluorophenyl)-1-(1-methylethyl)-3-phenyl-1H-pyrrol-2-yl]carbonyl)amino]methyl]benzoic acid
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7-[3,4-bis(4-fluorophenyl)-1-(1-methylethyl)-5-(phenylcarbamoyl)-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
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7-[3,4-bis(4-fluorophenyl)-5-[(3-hydroxyphenyl)carbamoyl]-1-(1-methylethyl)-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
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7-[3,4-bis(4-fluorophenyl)-5-[(3-methoxyphenyl)carbamoyl]-1-(1-methylethyl)-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
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7-[3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-5-(phenylcarbamoyl)-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
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7-[3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-5-(propylcarbamoyl)-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
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7-[3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-5-[(4-sulfamoylphenyl)carbamoyl]-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
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7-[3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-5-[(pyridin-2-ylmethyl)carbamoyl]-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
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7-[3-(4-fluorophenyl)-1-(1-methylethyl)-5-[[(4-methyl-1,3-thiazol-2-yl)methyl]carbamoyl]-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
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7-[3-(4-fluorophenyl)-1-(1-methylethyl)-5-[[(5-methyl-1H-imidazol-2-yl)methyl]carbamoyl]-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
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7-[3-(4-fluorophenyl)-1-(1-methylethyl)-5-[[(5-methyl-1H-pyrazol-3-yl)methyl]carbamoyl]-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
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7-[3-(4-fluorophenyl)-5-(methylcarbamoyl)-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
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7-[3-(4-fluorophenyl)-5-[(4-hydroxyphenyl)carbamoyl]-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
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7-[3-(4-fluorophenyl)-5-[(4-methoxybenzyl)carbamoyl]-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
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7-[5-(benzylcarbamoyl)-3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
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7-[5-(cyclopropylcarbamoyl)-3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
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7-[5-(dimethylcarbamoyl)-3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
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7-[5-(ethylcarbamoyl)-3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
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7-[5-carbamoyl-3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
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7-[5-ethylcarbamoyl-3-(4-fluoro-phenyl)-1-isopropyl-4-pyridin-2-yl-1H-pyrrol-2-yl]-3,5-dihydroxy-heptanoicacid sodium salt
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7-[5-[(4-carbamoylphenyl)carbamoyl]-3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
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7-[5-[(4-carboxyphenyl)carbamoyl]-3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
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7-[5-[[(1,5-dimethyl-1H-pyrazol-3-yl)methyl]carbamoyl]-3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
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7-[5-[[3-(dimethylcarbamoyl)phenyl]carbamoyl]-3,4-bis(4-fluorophenyl)-1-(1-methylethyl)-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
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7-[5-[[4-(dimethylcarbamoyl)phenyl]carbamoyl]-3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
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8-hydroxygeraniol
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competitive inhibition mechanism, binds at the catalytic site, docking experiments, overview
adenosine-2'-monophospho-5'-diphosphoribose
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competitive inhibitor for NADPH binding site
alpha-asarone
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9.4% inhibition at 0.1 mM
brutieridin
i.e. hesperetin 7-(2''-alpha-rhamnosyl-6''-(3''''-hydroxy-3''''-methylglutaryl)-beta-D-glucoside), a flavonoid conjugate from bergamot fruit extract, structural analogue of statins, computational study, overview
ceramide
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treatment with exogenous ceramides, or increasing the endogenous ceramide levels inhibits HMGCR by 6080%
CoA disulfide
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no inactivation in presence of NADPH 1 mM, or HMG-CoA 0.5 mM
daidzein
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isoflavone, isolated and purified from korean soybean paste, structural analysis
digitonine
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2% digitonin, 80% inhibition
EDTA
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inhibits the subsequent reactions of the mevalonate pathway in Hevea latex
eicosapentaenoic acid
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inhibits translation of the enzyme about 50% at 0.15 mM, downregulation, slightly increases downregulation of protein synthesis by cycloheximide
F(4-fluoro)VAE
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HMG-CoA competitive inhibitor
FVAE
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HMG-CoA competitive inhibitor
genistein
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isoflavone, isolated and purified from korean soybean paste, structural analysis
GFPDGG
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designed on the basis of the rigid peptide backbone, increases the inhibitory potency more than 300 times compared to the first isolated LPYP from soybean, overview
GFPEGG
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HMG-CoA competitive inhibitor
GLPDGG
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NADPH and HMG-CoA competitive inhibitor
GLPEGG
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NADPH and HMG-CoA competitive inhibitor
glycitein
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isoflavone, isolated and purified from korean soybean paste, structural analysis
IAVE
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HMG-CoA competitive inhibitor
IAVP
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NADPH competitive inhibitor
IAVPGEVA
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isolated from soybean by pepsin
Ile-Ala-Val-Pro-Gly-Glu-Val-Ala
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IVAE
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HMG-CoA competitive inhibitor
melitidin
i.e. naringenin 7-(2''-alpha-rhamnosyl-6''-(3''''-hydroxy-3''''-methylglutaryl)-beta-D-glucoside), a flavonoid conjugate from bergamot fruit extract, structural analogue of statins, computational study, overview
methyl (2-methoxy-5-nitro-4-propylphenoxy)acetate
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96.8% inhibition at 0.1 mM
methyl (4-ethyl-2-nitrophenoxy)acetate
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84.9% inhibition at 0.1 mM
Mevinolin
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competitive with 3-hydroxy-3-methylglutaryl-CoA
myriocin
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concomitant reduction of both HMGR activity and the sterol content by depletion of the sphingolipid pathway. At 0.01 mM myriocin decrease to ca. 55% of the HMGR activity in control plants. Myriocin-induced down-regulation of HMGR activity is exerted at the post-translational level, like the regulatory response of HMGR to enhancement or depletion of the flux through the sterol pathway
p-chloromercuribenzoate
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1 mM, complete inhibition
resveratrol
inhibits the cell growth as well as the activity of recombinant enzyme. Resveratrol shows antitrypanosomal activity with an IC50 value of 0.00013 mM and moderate antipromastigote activity against Leishmania major with IC50 value: 0.153 mM
SFGYVAE peptide
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most active inhibitory peptide; shows high ability to inhibit HMGR by competitive inhibition with respect to (S)-3-hydroxy-3-methylglutaryl-CoA
small heterodimer partner nuclear receptor
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directly regulates cholesterol biosynthesis through inhibition of 3-hydroxy-3-methylglutaryl coenzyme A reductase
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SMase C
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treatment of fibroblasts with SMase C results in a 90% inhibition of HMGCR
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SMase D
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treatment of fibroblasts with SMase D inhibits by 29%
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sodium (E,3R,5S)-7-(2-(2-fluorophenyl)-4-(3-phenylpentan-3-yl)phenyl)-3,5-dihydroxy-hept-6-enoate
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has almost no effect on the activity
sodium (E,3R,5S)-7-(2-(3-fluorophenyl)-4-(3-phenylpentan-3-yl)phenyl)-3,5-dihydroxy-hept-6-enoate
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sodium (E,3R,5S)-7-(2-(4-fluorophenyl)-4-(3-phenylpentan-3-yl)phenyl)-3,5-dihydroxy-hept-6-enoate
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shows the most potent inhibitory activity among compounds comparable with that of clinically useful mevastatin
sodium (E,3R,5S)-7-(2-phenyl-4-(3-phenylpentan-3-yl)phenyl)-3,5-dihydroxyhept-6-enoate
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has almost no effect on the activity
sodium (E,3R,5S)-7-(4-(3-(2-fluorophenyl)pentan-3-yl)-2-isopropylphenyl)-3,5-dihydroxyhept-6-enoate
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sodium (E,3R,5S)-7-(4-(3-(3-fluorophenyl)pentan-3-yl)-2-isopropylphenyl)-3,5-dihydroxyhept-6-enoate
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sodium (E,3R,5S)-7-(4-(3-phenylpentan-3-yl)-2-isopropylphenyl)-3,5-dihydroxyhept-6-enoate
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squalestatin
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mutant plants, not wild-type plants, become sterile
YAVE
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HMG-CoA competitive inhibitor
YVAE
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HMG-CoA competitive inhibitor
atorvastatin
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atorvastatin
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has a differentiating effect on wild-type and mutant forms of the human protein
atorvastatin
inhibits the cell growth as well as the activity of recombinant enzyme, 315.5 nM are enough to cause 50% recombinant LdHMGR enzyme inhibition, 93.2% inhibition at 0.001 mM
cerivastatin
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cerivastatin
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biphasic inhibition mechanism, slow, tight-binding type of inhibitor
CoASH
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Compactin
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competitive inhibitor for HMG-CoA binding site
cycloheximide
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downregulation of protein synthesis, synergistic with eicosapentanoic acid and myristic acid
fluvastatin
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fluvastatin
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has a differentiating effect on wild-type and mutant forms of the human protein
fluvastatin
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competitive inhibitor
fluvastatin
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competitive
GFPTGG
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HMG-CoA competitive inhibitor; NADPH and HMG-CoA competitive inhibitor
GFPTGG
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competitive, effects on enzyme Michaelis-Menten kinetics, overview
GLPTGG
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NADPH and HMG-CoA competitive inhibitor
Hydroxymethylglutarate
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2 mM, slightly inhibitory
Hydroxymethylglutarate
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lovastatin
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lovastatin
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no effect of lovastatin on the growth curve of Hortaea werneckii in salt-free media, whereas remarkably reduced growth in the otherwise physiologically optimal medium containing 17% NaCl, an effect even more pronounced in hypersaline medium containing 25% NaCl. Inhibition of HMGR in vivo by lovastatin impairs the halotolerant character
lovastatin
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the representative of the statin class of drugs that in their active hydrolysed form are specific inhibitors of the enzyme
lovastatin
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slightly inhibitory statin for class II enzyme, binding structure at the active site involves the residues Lys267, Asn271, Glu83, Arg261, and 2 water molecules, substrate mimicking binding mode
lovastatin
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competitive inhibitor for HMG-CoA binding site
lovastatin
competitive inhibitor for HMG-CoA binding site
lovastatin
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competitive inhibitor for HMG-CoA binding site and noncompetitive inhibitor for NADPH binding site
mevastatin
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MgATP2-
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4 mM
p-hydroxymercuribenzoate
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0.01 mM inhibited 97% of reduction
p-hydroxymercuribenzoate
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3.7 mM, complete inhibition
pravastatin
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pravastatin
inhibitory in the presence of increasing concentrations of NADPH, but increasing concentrations of HMG-CoA block the HMG-CoA reductase-inhibiting activity
rosuvastatin
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thermodynamics of binding and inhibition mechanism, Glu559 is involved, reversible, 2-step complex formation, competitive with respect to 3-hydroxy-3-methylglutaryl-CoA, non-competitive to NADPH
simvastatin
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simvastatin
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does not allow differentiation between the wild-type and mutant forms of the human protein
simvastatin
inhibits the cell growth as well as the activity of recombinant enzyme, 63% inhibition at 0.1 mM
simvastatin
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enzyme inhibition causes 40% reduction of wound healing, inhibition of HMGR activity during acute wound healing interferes with keratinocyte VEGF production and proliferation at the wound site, overview
additional information
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whether plants are grown with mevalonate from the beginning or only during the last 9 days, HMGR activity is drastically reduced to 25% of the activity in plants grown in the absence of mevalonate. Plants grown without mevalonate during the last 9 days show a severe, though less pronounced, reduction in HMGR activity, which decreases to 60% of the activity in control plants. Significant reduction of HMGR activity does not correlate with changes in both the expression of HMG1 and HMG2 genes and the amount of HMGR protein
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additional information
no inhibition by farnesoate and farnesoic acid
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additional information
no inhibition by farnesoate and farnesoic acid
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additional information
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no inhibition by farnesoate and farnesoic acid
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additional information
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27-hydroxycholesterol strongly supresses the expression of HMGR, the in vivo inhibition of sterol 27-hydroxylase CYP27A1, e.g. by the drugs rapamycin and cyclosporine A, reduces the inhibition and thus increases HMGR activity, overview
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additional information
screening of eight-membered medium ring lactams and related tricyclic compounds, either seven-membered lactams, thiolactams or amines, for inhibitory potency, overview. The compounds are inhibitory also in the presence of increasing concentrations of NADPH, and are not affected by increasing concentrations of HMG-CoA. Medium ring lactams and existing statins may have different mechanisms of enzyme interaction and inhibition, molecular docking studies and comparisons using the HMG-CoA reductase statin-binding receptor model, overview. The ligands may occupy a narrow channel housing the pyridinium moiety on NADP+
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additional information
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screening of eight-membered medium ring lactams and related tricyclic compounds, either seven-membered lactams, thiolactams or amines, for inhibitory potency, overview. The compounds are inhibitory also in the presence of increasing concentrations of NADPH, and are not affected by increasing concentrations of HMG-CoA. Medium ring lactams and existing statins may have different mechanisms of enzyme interaction and inhibition, molecular docking studies and comparisons using the HMG-CoA reductase statin-binding receptor model, overview. The ligands may occupy a narrow channel housing the pyridinium moiety on NADP+
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additional information
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methanolic extracts of Quercus infectoria galls, Rosa damascena flowers, and Myrtus communis leaves inhibit the enzyme activity noncompetitively to 84%, 70%, and 62%, respectively. Extracts of diverse other plants are also inhibitory for the enzyme, detailed overview
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additional information
statins are potent enzyme inhibitors that bind to the active site where also the natural substrate binds, used widely in the treatment of hypercholesterolemia
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additional information
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design of highly potent and competitive inhibitory peptides for 3-hydroxy-3-methylglutaryl CoA reductase, no inhibition with SFGYVAG peptide
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additional information
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the activity of microsomal isoyzme Hmg2 is highest under hypo-saline and extremely hyper-saline conditions, and down-regulated under optimal growth conditions
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additional information
exogenous supplementation of ergosterol in case of atorvastatin and resveratrol treated cells causes complete reversal of growth inhibition whereas simvastatin is ergosterol refractory
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additional information
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exogenous supplementation of ergosterol in case of atorvastatin and resveratrol treated cells causes complete reversal of growth inhibition whereas simvastatin is ergosterol refractory
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additional information
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inhibition potency of inhibitors in hepatocytes, myocytes and on purified enzyme, overview
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additional information
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no inhibition by geraniol or by its glucoside and thioglucoside
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additional information
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discovery, synthesis, and optimization of substituted pyrrole-based hepatoselective ligands as potent inhibitors of HMG-CoA reductase for reducing low density lipoprotein cholesterol (LDL-c) in the treatment of hypercholesterolemia
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additional information
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design, synthesis and evaluation of structure-based peptide inhibitors, computational methods, overview
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additional information
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(E,3R,5S)-7-(4-(3-(4-fluorophenyl)pentan-3-yl)phenyl)-3,5-dihydroxyhept-6-enoic acid shows no apparent HMGR inhibitory activity even at 100 mM
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additional information
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the hybrid is resistant to race 0 of Phytophtora infestans
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