基于胰高血糖素类肽1受体的2型糖尿病治疗药物研究进展

胰高血糖素类肽(GLP-1)和葡萄糖依赖性促胰岛素多肽(GIP)为肠内分泌细胞在机体摄入营养时分泌的激素，因其能促进胰岛素的分泌和维持血糖的动态平衡，又被称为肠促胰素。而机体内广泛存在的二肽基肽酶-4(DPP-4)可快速灭活GLP-1和GIP，因此抑制DPP-4的活性可增强GLP-1和GIP激素的活性水平，从而改善2型糖尿病（T2DM）患者的胰岛功能和血糖控制，越来越多基于该靶点的药物被开发出来用于治疗2型糖尿病。本文综述了近年来国内外相关文献，阐述了肠促胰岛素与T2DM之间的关系，并介绍GLP－1发挥效应的机制、以及GLP类降糖药物、DPP-4抑制剂的开发设计原理。

Recent progress in research of antidiabetic agents for T2DM based on GLP-1 receptor

The peptides, glucagon-like peptide-1 (GLP-1) and Glucose-dependent insulinotropic polypeptide, are two kinds of incretin hormones secreted by the endocrine cells of gut following nutrient absorbed. These two peptides are also called incretin, and the function of them is to promote the secretion of insulin and maintain glucose homeostasis. Because they can be quickly inactivated by Dipeptidyl peptidase -4 (DPP-4) that is widely existing in the body, inhibit the active of DPP-4 can increase the function of GLP-1 and GIP. Thereby the Islet function and glycemic controlling for T2DM will be improved. more and more drugs based on the new target are developed to use for T2DM treatment. In this review, we discuss the relationship between incretin and T2DM, and the function mechanism of GLP-1, and drugs development for T2DM such as GLP-1 mimics and DPP-4 inhibitors.