Mayo Clinic, Rochester, Minnesota 55905, USA.
Curr Opin Gastroenterol. 2011 May;27(3):285-8. doi: 10.1097/MOG.0b013e32834452c8.
This review will provide an overview of the role of nuclear receptors in bile acid homeostasis with a focus on the farnesoid X receptor (FXR) and its potential therapeutic use in cholestatic liver diseases.
Nuclear receptors have emerged as important mediators of a variety of metabolic and transport functions involving the liver. The role of FXR, in particular, has come to light because of its important role in bile acid homeostasis. The use of potent FXR ligands has recently been shown to offer potentially important therapeutic benefits in patients with primary biliary cirrhosis, an important cholestatic liver disease of adults. This recent finding has now opened the door for future therapeutic trials for use of FXR agonists such as obeticholic acid for the treatment of chronic cholestatic liver diseases.
Further understanding of the role of farnesoid X receptor agonists and the potential role of ligands in animal models of other forms of cholestasis will be important to set the stage for future applications to human disease.
本篇综述旨在概述核受体在胆汁酸稳态中的作用，重点介绍法尼醇 X 受体（FXR）及其在胆汁淤积性肝病中的潜在治疗用途。
核受体已成为涉及肝脏的多种代谢和转运功能的重要调节剂。特别是 FXR 的作用已经凸显出来，因为它在胆汁酸稳态中起着重要作用。最近的研究表明，使用有效的 FXR 配体可能为原发性胆汁性肝硬化患者（成人重要的胆汁淤积性肝病）带来潜在的重要治疗益处。这一最新发现为未来使用 FXR 激动剂（如奥贝胆酸）治疗慢性胆汁淤积性肝病的治疗试验开辟了道路。
进一步了解法尼醇 X 受体激动剂的作用以及配体在其他形式胆汁淤积动物模型中的潜在作用，对于为将来在人类疾病中的应用奠定基础非常重要。
