孕烷X受体及组成性雄甾烷受体的研究新进展

Advances in the research of pregnane X receptor and constitutive androstane receptor

孕烷受体(pregnane X receptor,PXR)和组成性雄甾烷受体(constitutive androstane receptor,CAR)是核受体(nuclear receptor,NR)亚家族的重要成员;为配体活化的转录因子,能调控大量的靶基因。本文主要对其基本结构、机制及参与转录活化的辅助因子作简要介绍,重点讲述了它们在调节药物代谢与转运、糖异生及生酮作用、脂质代谢以及炎症反应等方面的意义。通过对PXR及CAR的研究,可以有效预测和防止药物相互作用;为寻找疾病治疗新靶标提供方向。

Nuclear receptors pregnane X receptor（PXR） and constitutive androstane receptor（CAR） are originally characterized as transcription factors regulating many target genes.Recent works have revealed that these nuclear receptors play critical roles in regulating genes that encode drug metabolism enzymes and modulating hepatic energy metabolism,such as down-regulating gluconeogenesis,fatty acid oxidation,and ketogenesis,as well as up-regulating lipogenesis.Studies on PXR and CAR have important implication on drug-drug interaction（DDI） and potential disease treatment targets.