TY - JOUR T1 - Glucuronidation of 3'-azido-3'-deoxythymidine by rat and human liver microsomes. JF - Drug Metabolism and Disposition JO - Drug Metab Dispos SP - 369 LP - 372 VL - 18 IS - 3 AU - E M Cretton AU - D V Waterhous AU - R Bevan AU - J P Sommadossi Y1 - 1990/05/01 UR - http://dmd.aspetjournals.org/content/18/3/369.abstract N2 - The glucuronidation of 3'-azido-3'-deoxythymidine (AZT) by rat and human liver microsomes has been studied in vitro. The AZT-glucuronide was preliminarily identified through specific hydrolysis by beta-glucuronidase and rigorous product identification was performed by high-field proton nuclear magnetic resonance and fast-atom-bombardment mass spectrometry. A beta-linked 5'-O-glucuronide was the exclusive product formed in liver microsomes. Rat and human liver microsomal uridine 5'-diphosphoglucuronyltransferase activities toward AZT were investigated. These studies revealed that AZT had a lower Km and a 5-6-fold higher relative catalytic efficiency for uridine 5'-diphosphoglucuronyltransferase in human as compared to rat liver microsomes which may play a role in the quantitative differences observed in the degree of AZT glucuronidation between rat and human. ER -