组成型雄烷受体的小分子调节剂
Small-molecule modulators of the constitutive androstane receptor.
作者信息
Cherian Milu T, Chai Sergio C, Chen Taosheng
机构信息
Postdoctoral fellow, St. Jude Children's Research Hospital, Department of Chemical Biology and Therapeutics , 262 Danny Thomas Place, Memphis, TN 38105 , USA.
出版信息
Expert Opin Drug Metab Toxicol. 2015 Jul;11(7):1099-114. doi: 10.1517/17425255.2015.1043887. Epub 2015 May 15.
Abstract
INTRODUCTION
The constitutive androstane receptor (CAR) induces drug-metabolizing enzymes for xenobiotic metabolism.
AREAS COVERED
This review covers recent advances in elucidating the biological functions of CAR and its modulation by a growing number of agonists and inhibitors.
EXPERT OPINION
Extrapolation of animal CAR function to that of humans should be carefully scrutinized, particularly when rodents are used in evaluating the metabolic profile and carcinogenic properties of clinical drugs and environmental chemicals. Continuous efforts are needed to discover novel CAR inhibitors, with extensive understanding of their inhibitory mechanism, species selectivity, and discriminating power against other xenobiotic sensors.
摘要
引言
组成型雄烷受体（CAR）可诱导药物代谢酶参与外源性物质的代谢。
涵盖领域
本综述涵盖了在阐明CAR的生物学功能及其被越来越多的激动剂和抑制剂调节方面的最新进展。
专家观点
将动物CAR功能外推至人类时应仔细审查，特别是在使用啮齿动物评估临床药物和环境化学物质的代谢谱及致癌特性时。需要持续努力发现新型CAR抑制剂，并深入了解其抑制机制、物种选择性以及对其他外源性物质传感器的区分能力。
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Chrysin, baicalein and galangin are indirect activators of the human constitutive androstane receptor (CAR).白杨素、黄芩素和高良姜素是人类组成型雄甾烷受体（CAR）的间接激活剂。
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Developing Adnectins that target SRC co-activator binding to PXR: a structural approach toward understanding promiscuity of PXR.研发针对 SRC 共激活子结合 PXR 的 Adnectin：一种理解 PXR 混杂性的结构方法。
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