GLP-1R激动剂及正变构调节剂研究进展  

Research progress in GLP-1R agonists and positive allosteric modulators

作　　者：王芮 杨紫鑫 宋士奎 柯志强 苏正定[1] WANG Rui;YANG Zixin;SONG Shikui;KE Zhiqiang;SU Zhengding(Cooperative Innovation Center of Industrial Fermentation(Ministry of Education&Hubei Province),Hubei University of Technology,Hubei Wuhan 430068,China;Wuhan Amersino Biodevelop Inc.,Biolake Park,Hubei Wuhan 430075,China;Hubei Key Laboratory for Diabetes and Angiopathy,Xianning Medical College,Hubei University of Science and Technology,Hubei Xianning 437100,China)

机构地区：[1]湖北工业大学工业发酵省部共建协同创新中心,湖北武汉430068 [2]武汉艾默佳华生物科技有限公司,湖北武汉430075 [3]湖北科技学院咸宁医学院,糖尿病心脑血管病变湖北省重点实验室,湖北咸宁437100

出　　处：《中国医院药学杂志》2023年第21期2453-2458,共6页Chinese Journal of Hospital Pharmacy

基　　金：教育厅科学研究计划指导性项目(编号:B2021224)。

摘　　要：胰高血糖素样肽-1受体(glucagon-like peptide-1 receptor,GLP-1R)是治疗2型糖尿病的重要靶标,作为一种G蛋白偶联受体可通过胰高血糖素样肽-1介导胰岛素分泌。该文对胰高血糖素样肽-1和GLP-1R的结构与功能进行综述,并对肽类GLP-1R激动剂、非肽类小分子GLP-1R激动剂和GLP-1R正变构调节剂的设计开发进行讨论,旨在为进一步探寻2型糖尿病的治疗方案提供思路。Glucagon-like peptide-1 receptor(GLP-1R)is an important target for the treatment of type 2 diabetes.It is a G protein-coupled receptor that mediates insulin secretion through glucagon-like peptide-1.The paper reviewed the structure and function of glucagon-like peptide-1 and GLP-1R,and the design and development of GLP-1R-like stimulants,non-peptide small molecule agonists and positive allosteric modulators of GLP-1R were discussed,so as to provide ideas for further exploring the treatment options for type 2 diabetes.

关 键 词：胰高血糖素样肽-1 胰高血糖素样肽-1受体 肽类GLP-1R激动剂 小分子GLP-1R激动剂 GLP-1R正变构调节剂 

分 类 号：R977.9[医药卫生—药品]