Title : Product inhibition of UDP-glucuronosyltransferase (UGT) enzymes by UDP obfuscates the inhibitory effects of UGT substrates.

Pub. Date : 2008 Feb

PMID : 17998297






2 Functional Relationships(s)
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1 In the present study, we found that UGT1A1-catalyzed estradiol 3-O-glucuronide formation and UGT1A4-catalyzed imipramine N-glucuronide formation in human liver microsomes were prominently decreased in the presence of 1-naphthol, but those by recombinant human UGT1A1 and UGT1A4, respectively, were not. 1-naphthol UDP glucuronosyltransferase family 1 member A4 Homo sapiens
2 Interestingly, when recombinant UGT1A6 was added in the reaction mixture, these activities by recombinant UGT1A1 and UGT1A4 were diminished in the presence of 1-naphthol. 1-naphthol UDP glucuronosyltransferase family 1 member A4 Homo sapiens