Lim Yun-Ping, Huang Jin-ding
Department of Pharmacology, Medical College, National Cheng Kung University, Tainan, Taiwan.
Drug Metab Pharmacokinet. 2008;23(1):14-21. doi: 10.2133/dmpk.23.14.
Human body needs to protect itself from a diverse array of harmful chemicals. These chemicals are also involved in drug metabolism, enzyme induction, and can cause adverse drug-drug interactions. Being a member of nuclear receptors (NRs), pregnane X receptor (PXR) has recently emerged as transcriptional regulators of cytochrome P450 (CYP) and transporters expression so as to against xenobiotics exposure. This review describes some common nuclear receptors, i.e. farnesoid X receptor (FXR), small heterodimer partner (SHP), hepatocyte nuclear factor-4alpha (HNF-4alpha), liver X receptor (LXR), glucocorticoid receptor (GR), constitutive androstane receptor (CAR) that crosstalk with PXR and involvement of coregulators thus control target genes expression.
人体需要保护自身免受各种各样有害化学物质的侵害。这些化学物质还参与药物代谢、酶诱导,并可导致不良的药物相互作用。作为核受体(NRs)的一员,孕烷X受体(PXR)最近已成为细胞色素P450(CYP)和转运蛋白表达的转录调节因子,以抵御外源性物质暴露。本综述描述了一些常见的核受体,即法尼酯X受体(FXR)、小异二聚体伴侣(SHP)、肝细胞核因子-4α(HNF-4α)、肝X受体(LXR)、糖皮质激素受体(GR)、组成型雄烷受体(CAR),它们与PXR相互作用,并通过共调节因子的参与来控制靶基因的表达。