PXR/CAR-代谢酶/转运体解毒系统的功能及研究进展

doi:10.19803/j.1672-8629.20240065

摘要/Abstract

摘要： 目的综述孕烷X受体（PXR）和组成型雄甾烷受体（CAR）-代谢酶/转运体解毒系统的功能和研究进展。方法从肝脏代谢酶、肝肾转运体、PXR/CAR介导的药物解毒等多方面对PXR/CAR-代谢酶/转运体解毒系统及其在药物解毒方面的研究进展进行论述。结果与结论 药物作为人体外源性物质,可能存在一定毒副作用,使用不当或毒性较强的药物易造成机体损伤。药物代谢酶和转运体是决定药物体内过程及暴露量的两大核心因素,在药物毒性与解毒方面扮演重要角色。随着对PXR和CAR研究的不断深入,发现其对药物解毒相关的代谢酶和转运体发挥核心调控作用,共同构成了机体最重要的防御解毒系统—PXR/CAR-代谢酶/转运体解毒系统。

关键词: 孕烷X受体, 组成型雄甾烷受体, 代谢酶, 转运体, 药物解毒系统

Abstract: Objective To outline the functions of and research progress in the nuclear receptor pregnane X receptor (PXR) and constitutive androstane receptor (CAR)-metabolic enzyme/transporter detoxification system. Methods The detoxification system of PXR/CAR-metabolic enzyme/transporter and its applications were reviewed in terms of the liver metabolic enzyme, liver and kidney transporter and PXR CAR-mediated drug detoxification. Results and Conclusion Drugs, as exogenous substances in the human body, may have toxicity and side effects, which is likely to cause injury when administrated improperly or with apparent toxicity. Drug metabolic enzymes and transporters are two pivotal factors in determining the process and exposure of drugs in vivo, making much difference to drug toxicity and detoxification. With the continuous deeping of research, PXR and CAR have been found to play a central regulatory role in metabolic enzymes and transporters related to drug detoxification. As a result, PXR and CAR can combine with their related drug metabolizing enzymes and transporters to constitute the most important defense detoxification system in vivo, the so-called PXR/CAR- metabolic enzymes/transporters detoxification system.

Key words: PXR, CAR, metabolic enzymes, transporter, drug detoxification system

中图分类号:

秦佳琪, 张帆, 吕东霞, 贺震, 魏玉辉. PXR/CAR-代谢酶/转运体解毒系统的功能及研究进展[J]. 中国药物警戒, 2024, 21(6): 709-715.

QIN Jiaqi, ZHANG Fan, LYU Dongxia, HE Zhen, WEI Yuhui. Functions of PXR/CAR-metabolizing enzyme/transporter detoxification system and research progress[J]. Chinese Journal of Pharmacovigilance, 2024, 21(6): 709-715.

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