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核受体(NRs)是一种转录调控因子,能够在转录水平上对药物代谢酶和转运体的表达进行调控,其中雄甾烷受体(CAR)和孕甾烷受体(PXR)均属于核受体家族中的异源物核受体(XRs).XRs作为细胞传感器,能够接受各种内源和外源性物质的刺激,并调控药物代谢酶和转运体基因的转录水平.CAR和PXR都能够通过配体依赖(直接激活)和非配体依赖(间接激活)两种方式,被不同的化学物质激活,进而影响药物代谢酶和转运体的表达,对药物代谢过程进行调控.本文综述了CAR和PXR不同激活途径的信号通路,为临床药物代谢和药物相互作用研究提供参考.“,”Nuclear receptors (NRs) are transcription factors that govern the expression of drug metabolisms and transporters at the transcription level.Constitutive androstane receptor (CAR) and pregnane X receptor (PXR) belong to xenobiotic receptors (XRs) in the family of NRs.CAR and PXR act as cellular sensors to accept a variety of stimulus by endogenous metabolites or exogenous compound and regulate the transcription level of drug metabolisms and transporters.Both CAR and PXR can be activated through ligand-dependent (direct) and ligand-independent (indirect) manners by structurally unrelated chemicals,and thereby regulate the expression of drug metabolisms and transporters.This review summerizes different pathways associated with the two activation mechanisms of CAR and PXR,and provides references for clinical drug metabolisms study.