胰高血糖素样肽-1受体靶向药物研究进展  

Advances in the research of the drugs targeting glucagon-like peptide-1 receptor

作　　者：李彩娜[1] 申竹芳[1] 

机构地区：[1]中国医学科学院北京协和医学院药物研究所,北京100050

出　　处：《中国新药杂志》2009年第23期2219-2222,2232,共5页Chinese Journal of New Drugs

摘　　要：胰高血糖素样肽-1(Glucagon-like peptide-1,GLP-1)是一种肠道L细胞分泌的肠降糖素,由30个氨基酸组成。GLP-1与受体结合后具有一定的抗糖尿病作用,但其体内半衰期短(约2min),临床应用受限。GLP-1受体是目前开发抗糖尿病药物的新靶点之一,旨在寻找可以同时激动GLP-1受体和耐受二肽基肽酶IV降解的长效肽类或非肽类化合物。目前该类多肽中exenatide已被美国食品药品管理局批准上市,liraglutide等处于临床研究阶段,尚有很多肽类或非肽类化合物处于临床前研究阶段。文中将近几年来靶向GLP-1受体的研究成果综述如下。Glucagon-like peptide-1 （GLP-1） ,a 30 amino-acid peptide,is an incretin secreted from the intestinal L cells. It can bind to the GLP-1 receptor to exert a variety of anti-diabetic activity. However,its half-life is only about 2 min in vivo,which may limit its application in clinic. Even though, GLP-1 receptor remains to be a new target for the research and development of anti-diabetic drugs. The aim is to discover long-term peptidic or non-peptidic glucagon-like peptide-1 receptor agonists, which could also resist the degradation by dipeptidyl peptidase Ⅳ （ DPP Ⅳ）. Up to date, besides of exenatide that has been approved by US Food Drug Administration （ FDA）, there are some peptides,such as liraglutide,in clinic study state and many other peptidic or non-peptidic compounds in pre-clinie study state. In this article,we reviewed the recent achievements regarding drugs targeting GLP-1 receptor.

关 键 词：胰高血糖素样肽-1受体 靶向药物 EXENATIDE LIRAGLUTIDE 

分 类 号：R977.15[医药卫生—药品]