2.7.1.48: uridine/cytidine kinase
This is an abbreviated version!
For detailed information about uridine/cytidine kinase, go to the full flat file.
Word Map on EC 2.7.1.48
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2.7.1.48
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thymidine
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salvage
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uracil
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phosphoribosyltransferase
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phosphorylase
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orotate
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ump
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5-fluorouracil
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5-fluorouridine
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deoxycytidine
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5-azacytidine
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6-azauridine
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3-deazauridine
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orotidine
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pyrazofurin
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medicine
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5-fluoro-2'-deoxyuridine
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3huridine
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dihydrouracil
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drug development
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diagnostics
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biotechnology
- 2.7.1.48
- thymidine
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salvage
- uracil
-
phosphoribosyltransferase
- phosphorylase
- orotate
- ump
- 5-fluorouracil
- 5-fluorouridine
- deoxycytidine
- 5-azacytidine
- 6-azauridine
- 3-deazauridine
- orotidine
- pyrazofurin
- medicine
- 5-fluoro-2'-deoxyuridine
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3huridine
- dihydrouracil
- drug development
- diagnostics
- biotechnology
Reaction
Synonyms
ATP:uridine 5'-phosphotransferase, hsUCK2, kinase, uridine (phosphorylating), More, pyrimidine ribonucleoside kinase, ttCK, UCK, UCK1, UCK2, UCKL1, Udk, UK/UPRT1, uridine cytidine kinase 2, uridine kinase, uridine phosphokinase, uridine-cytidine kinase, uridine-cytidine kinase 2, uridine/cytidine kinase, uridine/cytidine kinase 2
ECTree
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Inhibitors
Inhibitors on EC 2.7.1.48 - uridine/cytidine kinase
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(1E)-[[4-(4-tert-butylphenyl)-5-cyano-6-hydroxypyrimidin-2-yl]sulfanyl]-N-(2-methoxyphenyl)ethanimidic acid
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(1Z)-[([5-[(4-fluorophenyl)methyl]-7-oxo-6,7-dihydro-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl]methyl)sulfanyl]-N-(2-methylphenyl)ethanimidic acid
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2-[(5-cyano-4-hydroxy-6-phenylpyrimidin-2-yl)sulfanyl]-N-(4-ethylphenyl)acetamide
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2-[[1-(4-fluorophenyl)-4-oxo-5H-pyrazolo[3,4-d]pyrimidin-6-yl]sulfanyl]-N-[2-(trifluoromethyl)phenyl]acetamide
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2-[[4-(4-tert-butylphenyl)-5-cyano-6-hydroxypyrimidin-2-yl]sulfanyl]-N-(4-chlorophenyl)acetamide
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3-(2-[[9-methoxy-2-(4-methylphenyl)-5H-[1]benzopyrano[2,3-d]pyrimidin-4-yl]sulfanyl]acetamido)benzoic acid
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3-(2-[[9-methyl-2-(4-methylphenyl)-5H-[1]benzopyrano[2,3-d]pyrimidin-4-yl]sulfanyl]acetamido)benzoic acid
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3-[[2-[[2-(4-fluorophenyl)-5H-chromeno[2,3-d]pyrimidin-4-yl]sulfanyl]acetyl]amino]benzoic acid
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4-(2-[[9-methyl-2-(4-methylphenyl)-5H-[1]benzopyrano[2,3-d]pyrimidin-4-yl]sulfanyl]acetamido)benzoic acid
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4-[[2-[[2-(4-methoxyphenyl)-5H-chromeno[2,3-d]pyrimidin-4-yl]sulfanyl]acetyl]amino]benzoic acid
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bhutkesoside A
isolated from Ligusticopsis wallichiana (Apiaceae). Hydrophobic interactions are predicted for bhutkesoside A with Phe83
bhutkesoside B
isolated from Ligusticopsis wallichiana (Apiaceae). Bhutkesoside B is estimated to inhibit UCK2 protein by binding to the catalytic active site of ATP, thus inhibiting ATP from binding to its active site in the UCK2 protein. Hydrophobic interactions are predicted for bhutkesoside B with Ala30
N-(3,5-dimethylphenyl)-2-[([5-[(4-fluorophenyl)methyl]-7-oxo-2,5,6,7-tetrahydro-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl]methyl)sulfanyl]acetamide
inhibits 3'-ethynylcytidine 5'-triphosphate (5-EU) salvage by about 40% at 0.05 mM
N-(4-bromophenyl)-2-[[1-(4-fluorophenyl)-4-hydroxy-1H-pyrazolo[3,4-d]pyrimidin-6-yl]sulfanyl]acetamide
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p-chloromercuribenzoate
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0.17 mM, 67% inhibition, 0.69 mM, 82% inhibition, glutathione protects
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0.6 mM, approx. 80% inhibition of soluble enzyme, complete inhibition of Pb2+-precipitated enzyme
CTP
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inhibition is partially lost upon ageing of the enzyme and CTP becomes effective as a phosphate donor
UTP
inhibition of wild-type ttCK Y93, no inhibition of mutant ttCK H93
establishment and miniaturization of an in vitro assay for UCK2 activity and high-throughput screen against an about 40,000-compound library to generate drug-like leads. Analysis of the structures, activities, and modes of inhibition of the most promising hits, overview. Non-competitive UCK2 inhibitors are identified which are able to suppress nucleoside salvage in cells both in the presence and absence of dihydroorotate dehydrogenase (DHODH) inhibitors. No inhibition by 2-[[9-methyl-2-(4-methylphenyl)-5H-[1]benzopyrano[2,3-d]pyrimidin-4-yl]sulfanyl]-N-phenylacetamide, and (1Z)-N-(4-fluorophenyl)[([5-[(4-fluorophenyl)methyl]-7-oxo-6,7-dihydro-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl]methyl)sulfanyl]ethanimidic acid
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additional information
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establishment and miniaturization of an in vitro assay for UCK2 activity and high-throughput screen against an about 40,000-compound library to generate drug-like leads. Analysis of the structures, activities, and modes of inhibition of the most promising hits, overview. Non-competitive UCK2 inhibitors are identified which are able to suppress nucleoside salvage in cells both in the presence and absence of dihydroorotate dehydrogenase (DHODH) inhibitors. No inhibition by 2-[[9-methyl-2-(4-methylphenyl)-5H-[1]benzopyrano[2,3-d]pyrimidin-4-yl]sulfanyl]-N-phenylacetamide, and (1Z)-N-(4-fluorophenyl)[([5-[(4-fluorophenyl)methyl]-7-oxo-6,7-dihydro-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl]methyl)sulfanyl]ethanimidic acid
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additional information
discovery of two diacetylene glycosides as human uridine-cytidine kinase 2 inhibitors, in an in silico approach. Molecular ligand-protein docking, using uridine-cytidine kinase 2 structure PDB ID 1UDW. Druggability likeliness property of Bhutkesoside A and Bhutkesoside B as GPCR ligands, ion channel modulators (ICM), kinase inhibitors (KI), nuclear receptor ligands (NRL), protease inhibitors (PI) and enzyme inhibitors (EI) are studied, and results are retrieved as bioactivity scores, overview
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additional information
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no substrate inhibition of cytidine and 5-fluorouridine at substrate concentrations higher than 0.5 mM
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