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Literature summary extracted from

  • Fujiwara, R.; Nakajima, M.; Yamanaka, H.; Katoh, M.; Yokoi, T.
    Product inhibition of UDP-glucuronosyltransferase (UGT) enzymes by UDP obfuscates the inhibitory effects of UGT substrates (2008), Drug Metab. Dispos., 36, 361-367.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.1.17 1-naphthol inhibitory effects on different isozymes with different substrates, overview; inhibitory effects on different isozymes with different substrates, overview; inhibitory effects on different isozymes with different substrates, overview Homo sapiens
2.4.1.17 1-naphthol O-glucuronide inhibitory effects on different isozymes with different substrates, overview; inhibitory effects on different isozymes with different substrates, overview; inhibitory effects on different isozymes with different substrates, overview Homo sapiens
2.4.1.17 additional information 1-naphthol, 2-naphthol, 4-nitrophenol, and 4-methylumbelliferone with high turnover rates show more potent inhibition of the activity in human liver microsomes compared with that by the recombinant UGT1A1, inhibitory effects of UDP on UGT, overview; 1-naphthol, 2-naphthol, 4-nitrophenol, and 4-methylumbelliferone with high turnover rates show more potent inhibition of the activity in human liver microsomes, inhibitory effects of UDP on UGT, overview; 1-naphthol, 2-naphthol, 4-nitrophenol, and 4-methylumbelliferone with high turnover rates show more potent inhibition of the activity in human liver microsomes, inhibitory effects of UDP on UGT, overview Homo sapiens
2.4.1.17 UDP strongly inhibits isozymes UGT1A1 and UGT1A4 in a competitive manner for the 5'-diphosphoglucuronic acid binding; strongly inhibits isozymes UGT1A1 and UGT1A4 in a competitive manner for the 5'-diphosphoglucuronic acid binding; strongly inhibits isozymes UGT1A1 and UGT1A4 in a competitive manner for the 5'-diphosphoglucuronic acid binding Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.4.1.17 microsome
-
 Homo sapiens
-
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.4.1.17 Mg2+
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.4.1.17 UDP-D-glucuronate + acceptor Homo sapiens
-
 UDP + acceptor beta-D-glucuronoside
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.4.1.17 Homo sapiens
-
 isozyme UGT1A1
-
2.4.1.17 Homo sapiens P19224 isozyme UGT1A6; isozyme UGT1A6
-
2.4.1.17 Homo sapiens P22310 isozyme UGT1A4; isozyme UGT1A4
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.4.1.17 liver
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.1.17 UDP-D-glucuronate + 1-naphthol reaction of isozyme UGT1A6 Homo sapiens UDP + 1-naphthyl beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-D-glucuronate + 2-naphthol
-
 Homo sapiens UDP + 2-naphthyl beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-D-glucuronate + 4-methylumbelliferone
-
 Homo sapiens UDP + 4-methylumbelliferyl beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-D-glucuronate + 4-nitrophenol
-
 Homo sapiens UDP + 4-nitrophenyl beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-D-glucuronate + acceptor
-
 Homo sapiens UDP + acceptor beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-D-glucuronate + estradiol reaction of isozyme UGT1A1 Homo sapiens UDP + estradiol 3-O-beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-D-glucuronate + imipramine reaction of isozyme UGT1A4 Homo sapiens UDP + imipramine N-beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-D-glucuronate + serotonin reaction of isozyme UGT1A6 Homo sapiens UDP + serotonin O-beta-D-glucuronoside
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.4.1.17 UDP-glucuronosyltransferase
-
 Homo sapiens
2.4.1.17 UGT
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.4.1.17 37
-
 assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.4.1.17 7.4
-
 assay at Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.4.1.17 0.007
-
 pH 7.4, 37°C, isozyme and UGT1A1 Homo sapiens UDP
2.4.1.17 0.047
-
 pH 7.4, 37°C, isozyme and UGT1A4 Homo sapiens UDP