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Literature summary for 2.4.1.17 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
Search for more literature for 2.4.1.17

Inhibitors

Inhibitors Comment Organism Structure
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
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
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
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

Localization Comment Organism GeneOntology No. Textmining
microsome
-
 Homo sapiens
-
-

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

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

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
 Homo sapiens
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
UDP-glucuronosyltransferase
-
 Homo sapiens
UGT
-
 Homo sapiens

Temperature Optimum [°C]

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

pH Optimum

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

IC50 Value

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