法尼醇X受体拮抗剂的研究进展

Advances in the development of farnesoid X receptor antagonists

摘要: 法尼醇X受体(FXR)属于核受体超家族一员，在胆汁酸、三酰甘油、葡萄糖等的动态平衡中发挥重要作用。FXR拮抗剂可通过提高胆固醇7α-羟化酶(CYP7A1)的活性而促进总胆固醇向胆汁酸转化，同时调节相关靶基因降低三酰甘油、低密度脂蛋白以及升高高密度脂蛋白水平。因此，FXR拮抗剂有望成为治疗高脂血症的新型药物。近年来，FXR拮抗剂的研究取得了较大进展，已获得多种结构类型的FXR拮抗剂。本文就近年来报道的FXR拮抗剂进行综述。

Abstract: Farnesoid X receptor(FXR), a member of the nuclear receptor superfamily, plays an important role on the regulating bile acid, lipid and glucose homeostasis. FXR antagonist can stimulate the conversion of total cholesterol into bile acid by improving the activity of CYP7A1. It can also reduce the content of triglyceride, low-density lipoprotein and increase that of high-density lipoprotein by regulating the relevant target genes. Considering the above facts, FXR antagonist is expected to become a potential drug to treat hyperlipidemia. In recent years, great progress has been made in the research on FXR antagonists with their various structural types having been obtained. This article introduces natural and synthetic FXR antagonists reported in recent years.