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Literature summary for 2.4.1.17 extracted from

  • Bratton, S.M.; Mosher, C.M.; Khallouki, F.; Finel, M.; Court, M.H.; Moran, J.H.; Radominska-Pandya, A.
    Analysis of R- and S-hydroxywarfarin glucuronidation catalyzed by human liver microsomes and recombinant UDP-glucuronosyltransferases (2012), J. Pharmacol. Exp. Ther., 340, 46-55.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.4.1.17

Cloned(Commentary)

Cloned (Comment) Organism
-
 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(R)-7-hydroxywarfarin substrate (S)-7-hydroxywarfarin, noncompetitive Homo sapiens
(R)-8-hydroxywarfarin substrate (S)-6-hydroxywarfarin, noncompetitive Homo sapiens
(S)-8-hydroxywarfarin substrate (R)-8-hydroxywarfarin, noncompetitive Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.044
-
 (R)-7-hydroxywarfarin isoform UGT1A10, pH 7.6, 37°C Homo sapiens
0.105
-
 (R)-8-hydroxywarfarin isoform UGT1A10, pH 7.6, 37°C Homo sapiens
0.13
-
 (R)-7-hydroxywarfarin isoform UGT1A1, pH 7.6, 37°C Homo sapiens
0.139
-
 (S)-8-hydroxywarfarin isoform UGT1A10, pH 7.6, 37°C Homo sapiens
0.16
-
 (S)-7-hydroxywarfarin isoform UGT1A10, pH 7.6, 37°C Homo sapiens
0.21
-
 (R)-6-hydroxywarfarin isoform UGT1A10, pH 7.6, 37°C Homo sapiens
0.23
-
 (S)-7-hydroxywarfarin isoform UGT1A1, pH 7.6, 37°C Homo sapiens
0.36
-
 (S)-6-hydroxywarfarin isoform UGT1A10, pH 7.6, 37°C 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.
(R)-6-hydroxywarfarin + UDP-alpha-D-glucuronate
-
 Homo sapiens (R)-6-hydroxywarfarin 6-O-beta-D-glucuronide + UDP
-
 ?
(R)-7-hydroxywarfarin + UDP-alpha-D-glucuronate
-
 Homo sapiens (R)-7-hydroxywarfarin 7-O-beta-D-glucuronide + UDP
-
 ?
(R)-8-hydroxywarfarin + UDP-alpha-D-glucuronate
-
 Homo sapiens (R)-8-hydroxywarfarin 8-O-beta-D-glucuronide + UDP
-
 ?
(S)-6-hydroxywarfarin + UDP-alpha-D-glucuronate
-
 Homo sapiens (S)-6-hydroxywarfarin 6-O-beta-D-glucuronide + UDP
-
 ?
(S)-7-hydroxywarfarin + UDP-alpha-D-glucuronate
-
 Homo sapiens (S)-7-hydroxywarfarin 7-O-beta-D-glucuronide + UDP
-
 ?
(S)-8-hydroxywarfarin + UDP-alpha-D-glucuronate
-
 Homo sapiens (S)-8-hydroxywarfarin 8-O-beta-D-glucuronide + UDP
-
 ?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.333
-
 isoform UGT1A10, substrate (S)-7-hydroxywarfarin, pH 7.6, 37°C Homo sapiens (R)-7-hydroxywarfarin
0.344
-
 isoform UGT1A10, substrate (R)-8-hydroxywarfarin, pH 7.6, 37°C Homo sapiens (S)-8-hydroxywarfarin
0.401
-
 isoform UGT1A10, substrate (S)-6-hydroxywarfarin, pH 7.6, 37°C Homo sapiens (R)-8-hydroxywarfarin

General Information

General Information Comment Organism
physiological function isoform UGT1A1 is involved in glucuronidation´of the main warfarin metabolites, including Rac-6- and 7-hydroxywarfarin and their R- and S-enantiomers in the liver Homo sapiens