Center for Pharmacogenetics, Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15261, USA.
Center for Pharmacogenetics, Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15261, USA; Department of Pharmacology and Chemical Biology, University of Pittsburgh, Pittsburgh, PA 15261, USA.
Biochim Biophys Acta Mol Basis Dis. 2021 Jun 1;1867(6):166101. doi: 10.1016/j.bbadis.2021.166101. Epub 2021 Feb 15.
Pregnane X receptor (PXR) and constitutive androstane receptor (CAR) are two nuclear receptors that are well-known for their roles in xenobiotic detoxification by regulating the expression of drug-metabolizing enzymes and transporters. In addition to metabolizing drugs and other xenobiotics, the same enzymes and transporters are also responsible for the production and elimination of numerous endogenous chemicals, or endobiotics. Moreover, both PXR and CAR are highly expressed in the liver. As such, it is conceivable that PXR and CAR have major potentials to affect the pathophysiology of the liver by regulating the homeostasis of endobiotics. In recent years, the physiological functions of PXR and CAR in the liver have been extensively studied. Emerging evidence has suggested the roles of PXR and CAR in energy metabolism, bile acid homeostasis, cell proliferation, to name a few. This review summarizes the recent progress in our understanding of the roles of PXR and CAR in liver physiology.
孕烷 X 受体 (PXR) 和组成型雄烷受体 (CAR) 是两种核受体，它们通过调节药物代谢酶和转运体的表达在异源生物解毒中起重要作用而广为人知。除了代谢药物和其他异源生物外，相同的酶和转运体还负责许多内源性化学物质（或内源性生物）的产生和消除。此外，PXR 和 CAR 在肝脏中均高度表达。因此，可以想象，PXR 和 CAR 通过调节内源性生物的动态平衡，具有影响肝脏病理生理学的巨大潜力。近年来，PXR 和 CAR 在肝脏中的生理功能已得到广泛研究。新出现的证据表明 PXR 和 CAR 在能量代谢、胆汁酸动态平衡、细胞增殖等方面发挥作用。本综述总结了我们对 PXR 和 CAR 在肝脏生理学中的作用的最新认识。
