作为2型糖尿病治疗药物的G蛋白偶联受体40激动剂研究进展  

Recent Research Advances in G-protein Coupled Receptor 40 Agonists as Therapeutic Agents for Type 2 Diabetes

作　　者：周牧星 杨凌云[1] 周金培[1] 张惠斌[1] 

机构地区：[1]中国药科大学江苏省抗代谢性疾病药物重点实验室,江苏南京210009

出　　处：《药学进展》2015年第1期13-22,共10页Progress in Pharmaceutical Sciences

基　　金：国家"重大新药创制"科技重大专项(No.2013ZX09301303-002);江苏省自然科学基金(No.BK 20141349)

摘　　要：2型糖尿病约占糖尿病总病例数的90%,目前研发的其新型治疗药物主要是通过调节糖代谢通路来控制血糖水平,它们可通过激活G蛋白偶联受体尤其是G蛋白偶联受体40,增强胰岛β细胞功能,促进胰岛素分泌,提高机体对胰岛素的敏感性,从而达到治疗糖尿病的目的。G蛋白偶联受体40作为抗2型糖尿病的新靶点,以其潜在优势,在糖尿病治疗领域备受关注。简介G蛋白偶联受体与其配体游离脂肪酸,重点综述不同结构的G蛋白偶联受体40激动剂的研究进展。Type 2 diabetes accounts for about 90% of all eases of diabetes. Novel therapeutic drugs for type 2 diabetes in current research and development control blood glucose level mainly by regulating glycometabolism pathways, which could strengthen the function of islet beta cells, promote insulin secretion and improve the body＇s sensitivity to insulin through activating G-protein coupled receptors（GPRs）, especially GPR40, so as to achieve the goal of treating diabetes. GPR40 as novel therapeutic targets for type 2 diabetes, with its potential advantages, has attracted much attention in the field of diabetes treatment. GPRs and Their ligands -free fatty acids were Introduced. The research progress on GPR40 agonists with different structures was especially reviewed.

关 键 词：G蛋白偶联受体40 激动剂 2型糖尿病 胰岛素分泌 血糖水平 

分 类 号：R977.15[医药卫生—药品]