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孕烷X受体在内源物质代谢中的功能

栾志琳, 霍笑笑, 管又飞^*, 张晓燕

大连医科大学医学科学研究院，大连 116044

摘要

核受体(nuclear receptor, NR)超家族成员孕烷X受体(pregnane X receptor, PXR)是一个配体激活型转录因子，高表达于肝脏和肠组织，在其它某些组织器官中也存在表达。PXR与维甲酸X受体(retinoid X receptor, RXR)形成异源二聚体，在招募大量共活化因子后，与特异性DNA响应元件结合发挥转录调控功能。PXR是一个公认的外源物质感受器，因此，PXR最初被认为是一种调节药物代谢酶和转运体的NR。但目前已知PXR也是同等重要的内源物质受体。最近的研究显示PXR激活可以调节体内葡萄糖代谢、脂质代谢、类固醇内分泌稳态、胆酸和胆红素去毒化、骨矿物质平衡和免疫炎症反应等，本文就这几个方面对PXR作一个综述。

关键词： 孕烷X受体; 转录调控; 内源物质; 代谢

分类号：R33

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

收稿日期：2018-06-05　　录用日期：2018-10-12

通讯作者：管又飞　　E-mail: guanyf@dmu.edu.cn

DOI: 10.13294/j.aps.2018.0080

引用本文：

栾志琳, 霍笑笑, 管又飞, 张晓燕. 孕烷X受体在内源物质代谢中的功能[J]. 生理学报 2019; 71 (2): 311-318.

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).