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Literature summary for 2.4.1.17 extracted from

  • Miller, G.P.; Lichti, C.F.; Zielinska, A.K.; Mazur, A.; Bratton, S.M.; Gallus-Zawada, A.; Finel, M.; Moran, J.H.; Radominska-Pandya, A.
    Identification of hydroxywarfarin binding site in human UDP glucuronosyltransferase 1A10: phenylalanine90 is crucial for the glucuronidation of 6- and 7-hydroxywarfarin but not 8-hydroxywarfarin (2008), Drug Metab. Dispos., 36, 2211-2218.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
-
Homo sapiens

Protein Variants

Protein Variants Comment Organism
F90A isoform 1A10, complete loss of activity to substrates 6- and 7-hydroxywarfarin, no change in activity to 8-hydroxywarfarin Homo sapiens
F93A increase in turnover rates for substrates 6- and 7-hydroxywarfarin, substrate inhibition kinetics Homo sapiens
V92A increase in turnover rates for substrates 6- and 7-hydroxywarfarin, substrate inhibition kinetics Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
6-hydroxywarfarin competitive Homo sapiens
7-hydroxywarfarin competitive Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.17
-
7-hydroxywarfarin wild-type, pH 7.4, 37°C Homo sapiens
0.19
-
8-hydroxywarfarin mutant F90A, pH 7.4, 37°C Homo sapiens
0.304
-
8-hydroxywarfarin mutant F93A, pH 7.4, 37°C Homo sapiens
0.39
-
8-hydroxywarfarin wild-type, pH 7.4, 37°C Homo sapiens
0.39
-
8-hydroxywarfarin mutant V92A, pH 7.4, 37°C Homo sapiens
0.48
-
6-hydroxywarfarin wild-type, pH 7.4, 37°C Homo sapiens
0.56
-
7-hydroxywarfarin mutant V92A, pH 7.4, 37°C Homo sapiens
0.7
-
6-hydroxywarfarin mutant V92A, pH 7.4, 37°C Homo sapiens
0.72
-
6-hydroxywarfarin mutant F93A, pH 7.4, 37°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
6-hydroxywarfarin + UDP-glucuronate
-
Homo sapiens ? + UDP
-
?
7-hydroxywarfarin + UDP-glucuronate
-
Homo sapiens ? + UDP
-
?
8-hydroxywarfarin + UDP-glucuronate
-
Homo sapiens ? + UDP
-
?

Synonyms

Synonyms Comment Organism
1A10
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.82
-
6-hydroxywarfarin mutant F93A, pH 7.4, 37°C Homo sapiens
1.1
-
6-hydroxywarfarin mutant V92A, pH 7.4, 37°C Homo sapiens
1.1
-
7-hydroxywarfarin mutant V92A, pH 7.4, 37°C Homo sapiens