中国临床药理学杂志2018,Vol.34Issue(10):1261-1264,4.DOI:10.13699/j.cnki.1001-6821.2018.10.035
异源物核受体激活机制在调控药物代谢中的研究现状
Research status on activation mechanisms of xenobiotic nuclear receptors mediated regulation of drug metabolisms
摘要
Abstract
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.关键词
异源物核受体/雄甾烷受体/孕甾烷受体/激活机制/药物代谢Key words
xenobiotic receptors/constitutive androstane receptor/pregnane X receptor/activation mechanism/drug metabolisms分类
医药卫生引用本文复制引用
徐艳娇,张思,鲁憬莉,张程亮,刘东..异源物核受体激活机制在调控药物代谢中的研究现状[J].中国临床药理学杂志,2018,34(10):1261-1264,4.基金项目
国家自然科学基金资助项目(81670521) (81670521)