Multiple forms of UDP-glucuronosyltransferase (UDPGTs) have been demonstrated in the livers of all mammalian species that have been studied. Rat liver possesses at least eight different isozymes and human liver has at least five different forms which have been identified. 2. Endogenous substrates (e.g., steroids) are helpful in distinguishing UDPGTs as they generally react with only a single form, whereas xenobiotic substrates (e.g., 4-methyl-umbelliferone, p-nitrophenol) react with several forms of the enzyme. 3. Human liver UDPGTs differ in physical properties and substrate specificity from these enzymes obtained from laboratory animals. Hence, it is necessary to study human liver UDPGTs to elucidate substrate specificity and to understand drug-endogenous substrate interaction in humans.
J Clin Invest. 1998 Feb 15;101(4):847-54. doi: 10.1172/JCI915.
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Pharmacokinetics and bioavailability of zidovudine and its glucuronidated metabolite in patients with human immunodeficiency virus infection and hepatic disease (AIDS Clinical Trials Group protocol 062).