以核受体为靶标的胆汁淤积治疗药物研究进展

摘要

Drug for cholestasis therapy is extremely limited.Ur-sodeoxycholic 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 re-presents a major goal for both pharmaceutical industry and aca-demic researchers.Targeting nuclear receptors in cholestasis is an intriguing approach since these receptors are critically in-volved in the regulation of bile acid homeostasis.This review summarizes the roles of individual nuclear receptors in cholestasis and evaluates their potential clinical application.%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。