Advance in research of orphan nuclear receptor-mediated regulation of UDP-glucuronosyltransferases

Abstract

Abstract: UDP-glucuronosyltransferases (UGTs) belong to the Phase II drug metabolizing enzymes.UGTs mediate transformations of glucuronic acid to xeno- and endobiotic chemicals, and it is the most important type of enzymes which involved in biotransformation of phase Ⅱ. More and more evidences have demonstrated that orphan nuclear receptors, such as pregnane X receptor (PXR), constitutive androstane receptor (CAR) and other transcriptional factors can regulate UGTs, differences of the factors above in distribution and activity can induce diversity of expression and activity of UGTs.Besides, researches indicated that the NR-mediated regulations of UGTs may contribute to variations of internal metabolism of compounds.In light of the expression of UGTs correlated to hormone homeostasis, therapeutic and side effects of medicine, incidence and prognosis of tumors and other diseases closely, therefore, elucidating UGT regulation by nuclear receptors has broad significance in drug interactions prediction and rational administration, human disease prevention and so on.

Key words: orphan nuclear receptor, gene regulation, UDP-glucuronosyltransferase

CLC Number:

R969
R968

ZHANG Li, ZHOU Hong-hao. Advance in research of orphan nuclear receptor-mediated regulation of UDP-glucuronosyltransferases[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2007, 12(9): 974-979.

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