Yan Jiong, Xie Wen
Center for Pharmacogenetics and Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15261, USA.
Center for Pharmacogenetics and Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15261, USA; Department of Pharmacology and Chemical Biology, University of Pittsburgh, Pittsburgh, PA 15261, USA.
Acta Pharm Sin B. 2016 Sep;6(5):450-452. doi: 10.1016/j.apsb.2016.06.011. Epub 2016 Jul 21.
The nuclear receptors pregnane X receptor (PXR) and constitutive androstane receptor (CAR) were cloned and/or established as xenobiotic receptors in 1998. Due to their activities in the transcriptional regulation of phase I and phase II enzymes as well as drug transporters, PXR and CAR have been defined as the master regulators of xenobiotic responses. The discovery of PXR and CAR provides the essential molecular basis by which drugs and other xenobiotic compounds regulate the expression of xenobiotic enzymes and transporters. This article is intended to provide a historical overview on the discovery of PXR and CAR as xenobiotic receptors.
核受体孕烷X受体（PXR）和组成型雄甾烷受体（CAR）于1998年被克隆和/或确立为外源性物质受体。由于它们在I相和II相酶以及药物转运体的转录调控中的作用，PXR和CAR已被定义为外源性物质反应的主要调节因子。PXR和CAR的发现为药物和其他外源性化合物调节外源性物质酶和转运体的表达提供了重要的分子基础。本文旨在对PXR和CAR作为外源性物质受体的发现进行历史概述。
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