Identification of selective inhibitors of uridine 5'-diphospho-glucuronosyltransferase (UGT) 1A3 and UGT1A8 and their application in UGT reaction phenotyping studies in human liver and intestinal microsomes.

Abstract excerpt

Uridine 5'-diphospho-glucuronosyltransferase (UGT) reaction phenotyping studies have posed significant challenges due to the limited availability of isoform-selective inhibitors. This recognized gap in reagent availability impedes the accurate determination of the contribution of specific UGT isoforms to the metabolism of UGT substrates. To address this challenge, 9 antibiotics were evaluated for their potential...

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