Use of transgenic mice in UDP-glucuronosyltransferase (UGT) studies

Abstract

Transgenic mouse models are useful to understand the function and regulation of drug-metabolizing enzymes in vivo. This article is intended to describe the general strategies and to discuss specific examples on how to use transgenic, gene knockout, and humanized mice to study the function as well as genetic and pharmacological regulation of UDP-glucuronosyltransferases (UGTs). The physiological and pharmacological implications of transcription factor–mediated UGT regulation will also be discussed. The UGT-regulating transcription factors to be discussed in this article include nuclear hormone receptors (NRs), aryl hydrocarbon receptor (AhR), and nuclear factor erythroid 2–related factor 2 (Nrf2).

Keywords::

• UGT
• transgenic mice
• humanized mice
• transcription factors
• gene regulation

Acknowledgements

The original research of ours described in this article was supported in part by NIH grants ES012479, CA 107011, and ES014626.

Declaration of interest: The authors declare no conflict of interest.