De Magalhaes Filho C Daniel, Downes Michael, Evans Ronald M
Gene Expression Laboratory, The Salk Institute for Biological Studies, La Jolla, Calif., USA.
Dig Dis. 2017;35(3):185-190. doi: 10.1159/000450909. Epub 2017 Mar 1.
Obesity and its associated diseases, including type 2 diabetes, have reached epidemic levels worldwide. However, available treatment options are limited and ineffective in managing the disease. There is therefore an urgent need for the development of new pharmacological solutions. The bile acid (BA) Farnesoid X receptor (FXR) has recently emerged as an attractive candidate. Initially described for their role in lipid and vitamin absorption from diet, BAs are hormones with powerful effects on whole body lipid and glucose metabolism. In this review, we focus on FXR and how 2 decades of work on this receptor, both in rodents and humans, have led to the development of drug agonists with potential use in humans for treatment of conditions ranging from obesity-associated diseases to BA dysregulation.
肥胖及其相关疾病，包括2型糖尿病，在全球范围内已达到流行程度。然而，现有的治疗选择有限，且在控制该疾病方面效果不佳。因此，迫切需要开发新的药物解决方案。胆汁酸（BA）法尼酯X受体（FXR）最近已成为一个有吸引力的候选靶点。最初，胆汁酸因其在饮食中脂质和维生素吸收方面的作用而被描述，它们是对全身脂质和葡萄糖代谢具有强大作用的激素。在本综述中，我们重点关注FXR，以及在啮齿动物和人类中对该受体长达20年的研究工作如何促成了具有潜在人类应用价值的药物激动剂的开发，这些激动剂可用于治疗从肥胖相关疾病到胆汁酸失调等各种病症。
