Cai Shi-Ying, Boyer James L
Liver Center, Department of Medicine, Yale University School of Medicine, P.O. Box 208019, New Haven, CT 06520-8019, USA.
Expert Opin Ther Targets. 2006 Jun;10(3):409-21. doi: 10.1517/14728222.10.3.409.
The nuclear farnesoid X receptor (FXR) plays a pivotal role in maintaining bile acid homeostasis by regulating key genes involved in bile acid synthesis, metabolism and transport, including CYP7A1, UGT2B4, BSEP, MDR3, MRP2, ASBT, I-BABP, NTCP and OSTalpha-OSTbeta in humans. Altered expression or malfunction of these genes has been described in patients with cholestatic liver diseases. This review examines the rationale for the use of FXR ligand therapy in various cholestatic liver disorders and includes potential concerns.
核法尼醇X受体(FXR)通过调节参与胆汁酸合成、代谢和转运的关键基因,在维持胆汁酸稳态中发挥关键作用,这些基因在人类中包括CYP7A1、UGT2B4、BSEP、MDR3、MRP2、ASBT、I-BABP、NTCP和OSTα-OSTβ。胆汁淤积性肝病患者中已描述了这些基因的表达改变或功能异常。本综述探讨了在各种胆汁淤积性肝病中使用FXR配体疗法的基本原理,并包括潜在的问题。