核受体FXR的配体及复合物结构研究进展

Progress in the ligands and their complex structures of farnesoid X receptor

法尼醇X受体(FXR)属于核受体超家族,与代谢综合征的形成以及葡萄糖在体内的动态平衡等过程密切相关,是研发代谢疾病和抗糖尿病药物的重要靶标。近几年,FXR的激动剂、拮抗剂以及晶体结构等方面的研究有了较快的发展。本文综述了目前报道的不同类型的FXR配体及其构效关系,以及FXR复合物晶体结构的最新进展。

Farnesoid X receptor（FXR） belongs to the nuclear receptor superfamily.It is highly related to the formation of metabolic syndrome and the glucose homeostasis,and therefore represents an important drug target against metabolic diseases and diabetes.In recent years,great progress has been made in the agonists,antagonists,and crystal structures of FXR.The diverse FXR ligands and their structure-activity relationship are reviewed in this article.The advances in the crystal structures of FXR in complex with different ligands are also introduced.