GLP-1R结构和功能及小分子药物筛选研究进展

doi:10.13560/j.cnki.biotech.bull.1985.2017.02.005

摘要/Abstract

摘要： 胰高血糖素样肽-1受体（glucagon-like peptide-1 receptor,GLP-1R）作为2-型糖尿病（T2DM）药物研发和治疗的靶点有着十分重要的临床意义。尽管通过结构生物学,蛋白质工程等方法和手段对于GLP-1R结构的研究有了较大突破。但是关于其全长结构解析,多肽结合受体的分子机理及受体激活的内在机制还不曾得到解决。近些年有关GLP-1R相关研究发展较快,简述了该受体的结构与功能以及已有的小分子药物先导化合物,并讨论GLP-1受体分子结构作用机制的发展方向及应用前景,旨为进一步探寻2型糖尿病的治疗方案提供有利的帮助。

关键词: GLP-1R, 分子结构, 小分子药物

Abstract: Glucagon-like peptide-1 receptor（GLP-1R）as an important target for type 2 Diabetes mellitus（T2DM）therapy,presents clinic significance. The breakthroughs on GLP-1R structures and functions have been made via structural biology and protein engineering. However,it is still unknown on the analysis of its full length structure,the molecular mechanism of polypeptide binding receptors,and the intrinsic mechanism of receptor activation. Owing to the rapid research progresses relating to GLP-1R,this article briefly describes the structure and function of the GLP-1 receptor and the leading compound of existing small molecule drugs,also discusses the developing direction and application prospects of action mechanism of the GLP-1 receptor molecule structure,aiming to provide structure base for the treatment of T2DM.

Key words: GLP-1R, molecular structure, small molecule drugs

胡中平, 程念, 杨帆, 苏正定. GLP-1R结构和功能及小分子药物筛选研究进展[J]. 生物技术通报, 2017, 33(2): 30-40.

HU Zhong-ping, CHENG Nian, YANG Fan, SU Zheng-ding. Research Progress on Structure and Function of GLP-1R and Screening for Small Molecule Drugs[J]. Biotechnology Bulletin, 2017, 33(2): 30-40.

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