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Literature summary extracted from

  • Bourcier, K.; Hyland, R.; Kempshall, S.; Jones, R.; Maximilien, J.; Irvine, N.; Jones, B.
    Investigation into UDP-glucuronosyltransferase (UGT) enzyme kinetics of imidazole- and triazole-containing antifungal drugs in human liver microsomes and recombinant UGT enzymes (2010), Drug Metab. Dispos., 38, 923-929.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.4.1.17
-
 Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.4.1.17 0.007
-
 ketoconazole isoform UGT1A4, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.028
-
 bifonazole isoform UGT1A4, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.035
-
 sulconazole isoform UGT1A4, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.059
-
 miconazole isoform UGT1A4, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.115
-
 econazole isoform UGT1A4, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.124
-
 tioconazole isoform UGT1A4, pH 7.4, 37°C Homo sapiens
2.4.1.17 0.261
-
 alprazolam isoform UGT1A4, pH 7.4, 37°C Homo sapiens
2.4.1.17 1.13
-
 voriconazole isoform UGT1A4, pH 7.4, 37°C Homo sapiens
2.4.1.17 1.667
-
 fluconazole isoform UGT2B7, pH 7.4, 37°C Homo sapiens

Localization

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

Organism

EC Number Organism UniProt Comment Textmining
2.4.1.17 Homo sapiens
-
-
-

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 alprazolam + UDP-alpha-D-glucuronate
-
 Homo sapiens alprazolam D-glucuronate + UDP
-
 ?
2.4.1.17 bifonazole + UDP-alpha-D-glucuronate
-
 Homo sapiens bifonazole D-glucuronate + UDP
-
 ?
2.4.1.17 econazole + UDP-alpha-D-glucuronate
-
 Homo sapiens econazole D-glucuronate + UDP
-
 ?
2.4.1.17 fluconazole + UDP-alpha-D-glucuronate
-
 Homo sapiens fluconazole D-glucuronate + UDP
-
 ?
2.4.1.17 itraconazole + UDP-alpha-D-glucuronate
-
 Homo sapiens ?
-
 ?
2.4.1.17 ketoconazole + UDP-alpha-D-glucuronate
-
 Homo sapiens ?
-
 ?
2.4.1.17 miconazole + UDP-alpha-D-glucuronate
-
 Homo sapiens miconazole D-glucuronate + UDP
-
 ?
2.4.1.17 additional information UGT1A4 is the main enzyme involved in the metabolism of all compounds tested except for fluconazole, which is mainly metabolized by UGT2B7, probably mediating its O-glucuronide metabolism. UGT1A3 is also involved in the metabolism of all imidazoles but not triazoles Homo sapiens ?
-
 ?
2.4.1.17 sulconazole + UDP-alpha-D-glucuronate
-
 Homo sapiens sulconazole D-glucuronate + UDP
-
 ?
2.4.1.17 tioconazole + UDP-alpha-D-glucuronate
-
 Homo sapiens tioconazole D-glucuronate + UDP
-
 ?
2.4.1.17 voriconazole + UDP-alpha-D-glucuronate
-
 Homo sapiens voriconazole D-glucuronate + UDP
-
 ?