New technologies for assessing UDP-glucuronosyltransferase (UGT) metabolism in drug discovery and development

UDP-glucuronosyltransferases (UGT) are important hepatic xenobiotic metabolizing enzymes. As with the cytochrome P450 class of enzymes, a multiplicity of UGT forms exists in human liver and extra-hepatic tissues. The lack of a comprehensive set of UGT-selective antibodies, substrates and inhibitors has limited the scope of studies that can be conducted with human liver preparations. The current status of the emerging in vitro tools for identifying important UGT isoforms in a given metabolic pathway will be the focus of this review.

Section editors:Charles L. Crespi – BD Biosciences, Woburn, MA, USAKenneth Thummel – University of Washington, Seattle, WA, USA