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Role of pregnane X receptor (PXR) in endobiotic metabolism

LUAN Zhi-Lin, HUO Xiao-Xiao, GUAN You-Fei^*, ZHANG Xiao-Yan

Advanced Institute for Medical Sciences, Dalian Medical University, Dalian 116044, China

Abstract

As a member of the nuclear receptor superfamily, the pregnane X receptor (PXR) is a ligand-activated transcription factor. PXR is highly expressed in liver and intestinal tissues, and also found in other tissues and organs, such as stomach and kidney. After heterodimerization with retinoid X receptor (RXR), PXR recruits numerous co-activating factors, and binds to specific DNA response elements to perform transcriptional regulation of the downstream target genes. As an acknowledged receptor for xenobiotics, PXR was initially considered as a nuclear receptor regulating drug metabolizing enzymes and transporters. However, nowadays, PXR has also been recognized as an important endobiotic receptor. Recent studies have shown that PXR activation can regulate glucose metabolism, lipid metabolism, steroid endocrine homeostasis, detoxification of cholic acid and bilirubin, bone mineral balance, and immune inflammation in vivo. This review focuses on the role of PXR in metabolism of endogenous substances.

Key words: pregnane X receptor; transcriptional regulation; endobiotics; metabolism

Received: 2018-06-05　　Accepted: 2018-10-12

Corresponding author: 管又飞　　E-mail: guanyf@dmu.edu.cn

DOI: 10.13294/j.aps.2018.0080

Citing This Article：

LUAN Zhi-Lin, HUO Xiao-Xiao, GUAN You-Fei, ZHANG Xiao-Yan. Role of pregnane X receptor (PXR) in endobiotic metabolism. Acta Physiol Sin 2019; 71 (2): 311-318 (in Chinese with English abstract).