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Literature summary for 2.4.1.17 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
Search for more literature for 2.4.1.17

Cloned(Commentary)

Cloned (Comment) Organism
-
 Homo sapiens

KM Value [mM]

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

Localization

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
alprazolam + UDP-alpha-D-glucuronate
-
 Homo sapiens alprazolam D-glucuronate + UDP
-
 ?
bifonazole + UDP-alpha-D-glucuronate
-
 Homo sapiens bifonazole D-glucuronate + UDP
-
 ?
econazole + UDP-alpha-D-glucuronate
-
 Homo sapiens econazole D-glucuronate + UDP
-
 ?
fluconazole + UDP-alpha-D-glucuronate
-
 Homo sapiens fluconazole D-glucuronate + UDP
-
 ?
itraconazole + UDP-alpha-D-glucuronate
-
 Homo sapiens ?
-
 ?
ketoconazole + UDP-alpha-D-glucuronate
-
 Homo sapiens ?
-
 ?
miconazole + UDP-alpha-D-glucuronate
-
 Homo sapiens miconazole D-glucuronate + UDP
-
 ?
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 ?
-
 ?
sulconazole + UDP-alpha-D-glucuronate
-
 Homo sapiens sulconazole D-glucuronate + UDP
-
 ?
tioconazole + UDP-alpha-D-glucuronate
-
 Homo sapiens tioconazole D-glucuronate + UDP
-
 ?
voriconazole + UDP-alpha-D-glucuronate
-
 Homo sapiens voriconazole D-glucuronate + UDP
-
 ?