以核受体为靶标的胆汁淤积治疗药物研究进展

Nuclear receptors as drug targets in cholestasis

胆汁淤积的治疗药物匮乏,熊去氧胆酸是目前唯一被FDA通过的治疗原发性胆汁性肝硬化的药物,但其药效却限于疾病早期,因此迫切需要开发新的胆汁淤积治疗药物。核受体能调控胆汁酸稳态,它作为胆汁淤积治疗的靶标是目前研究的热点。该综述对目前报道最多的核受体进行总结,分析其作为胆汁淤积药物治疗靶标的利弊及应用前景。

Drug for cholestasis therapy is extremely limited. Ursodeoxycholic acid is currently the only FDA approved drug to treat primary biliary cirrhosis,whereas its efficacy is limited to early stage of the disease. Therefore,developing novel drugs represents a major goal for both pharmaceutical industry and academic researchers. Targeting nuclear receptors in cholestasis is an intriguing approach since these receptors are critically involved in the regulation of bile acid homeostasis. This review summarizes the roles of individual nuclear receptors in cholestasis and evaluates their potential clinical application.