法尼醇 X 受体 (FXR) 是一种胆汁酸激活的核受体 (BAR)，主要在肝脏和肠道中表达。在配体结合后，FXR 调节参与胆汁酸合成、转运和重吸收代谢过程的关键基因，还参与碳水化合物和脂质的代谢。由于其重要的功能，FXR被认为是治疗胆汁酸相关肝病的有希望的药物靶点。随着奥贝胆酸 (OCA) 作为第一个靶向 FXR 的小分子的批准，许多其他小分子正在临床试验中进行评估。本综述总结了 FXR 的结构，尤其是其配体结合结构域，以及靶向 FXR 的小分子（包括激动剂和拮抗剂）的发展。

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Farnesoid X receptor (FXR) is a bile acid activated nuclear receptor (BAR) and is mainly expressed in the liver and intestine. Upon ligand binding, FXR regulates key genes involved in the metabolic process of bile acid synthesis, transport and reabsorption and is also involved in the metabolism of carbohydrates and lipids. Because of its important functions, FXR is considered as a promising drug target for the therapy of bile acid-related liver diseases. With the approval of obeticholic acid (OCA) as the first small molecule to target FXR, many other small molecules are being evaluated in clinical trials. This review summarizes the structures of FXR, especially its ligand binding domain, and the development of small molecules (including agonists and antagonists) targeting FXR.