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

作　　者：陈攀[1] 李晶洁[2] 陈杰[1] 

机构地区：[1]中山大学附属第一医院药学部临床药学室,广东广州510080 [2]中山大学附属第六医院,广东广州510655

出　　处：《中国药理学通报》2015年第9期1195-1198,共4页Chinese Pharmacological Bulletin

基　　金：广东省自然科学基金博士启动项目(No 2014A030310096)

摘　　要：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.

关 键 词：胆汁淤积 法尼酯X受体 孕烷X受体 组成性雄烷受体 1 25-二羟基维生素D3受体 糖皮激素受体 肝脏X受体 过氧化物酶体增殖物活化受体 转录因子-E2-相关因子2 

分 类 号：R-05[医药卫生] R392.11