法尼醇X受体拮抗剂及药理活性研究进展  

Advances in farnesoid X receptor antagonists and their pharmacological activities

作　　者：刘维伊 孙建国[1] 曹伟灵 王广基[1] 王洪 LIU Weiyi;SUN Jianguo;CAO Weiling;WANG Guangji;WANG Hong(Key Laboratory of Drug Metabolism&Pharmacokinetics,China Pharmaceutical University,Nanjing 210009,Jiangsu,China;Department of Pharmacy,Shenzhen Luohu Hospital Group People's Hospital,The third Affiliated Hospital of Shenzhen University,Shenzhen 518001,Guangdong,China)

机构地区：[1]中国药科大学,药物代谢动力学重点实验室,江苏南京210009 [2]深圳市罗湖医院集团罗湖区人民医院,深圳大学第三附属医院,药学部,广东深圳518001

出　　处：《中国临床药理学与治疗学》2020年第7期764-774,共11页Chinese Journal of Clinical Pharmacology and Therapeutics

基　　金：国家自然科学基金(81603194,81930109,81720108032,81421005);新药创制科技重大专项(2018ZX09711001-002-003,2018ZX09711002-001-004);中国药科大学“双一流”建设项目(CPU2018GF01,CPU2018GF09);中国药科大学天然药物活性组分与药效国家重点实验室自主课题资助项目(SKLNMZZ202001,SKLNMZZ202020);中央高校基本科研业务费专项资金(2632020ZD17);深圳市三名工程(SZSM201801060)。

摘　　要：法尼醇X受体(FXR)是核受体超家族的一员,具有广泛的生理病理功能,参与维持胆汁酸、糖、脂等的稳态,另外参与肿瘤的发生发展。因此,FXR转录活性调控是治疗多种疾病的重要策略,FXR激动剂的研发已取得突破性进展。近年来研究发现,FXR转录活性抑制对多种疾病具有积极的贡献,FXR拮抗剂的研发及其药理活性研究已取得较大进展。因此,本文就FXR拮抗剂及其药理活性研究进行综述。Farnesoid X receptor(FXR)is a member of the nuclear receptor superfamily.It has extensive physiological functions in maintaining homeostasis of bile acids,lipids,and glucose.It also participates in the development of various tumors.Therefore,regulation of its transcriptional activity is accepted as an important strategy for treatment of many diseases,and various FXR agonists have been developed.In recent years,it has been found that inhibition of FXR transcriptional activity also shows beneficial effects on various diseases,therefore several FXR antagonists have been developed and their pharmacological activities have been tested in preclinical animal models.This article provides an update review on FXR antagonists and their pharmacological activities.

关 键 词：法尼醇X受体 拮抗剂 药理活性 

分 类 号：R969.1[医药卫生—药理学]