Research Center, Dong-A Pharm. Co., Ltd., Yongin 446-905, Korea.
Arch Pharm Res. 2011 Jul;34(7):1041-3. doi: 10.1007/s12272-011-0721-z.
Glucagon-like peptide-1 (GLP-1) is the main member of the incretin family and stimulates insulin secretion by binding with its specific receptor on pancreatic β-cells. In addition, GLP-1 exerts broad beneficial effects on the glucose regulation by suppressing food intake and delaying stomach emptying. Now, long acting GLP-1 analogs including exenatide and liraglutide have been approved for the treatment of diabetes mellitus type 2, however long-term injection can limit their use for these chronic patients. In this report, the authors provide a review on the development of non-peptide GLP-1 receptor agonists and introduce a novel agonist DA-15864.
胰高血糖素样肽-1(GLP-1)是肠促胰岛素家族的主要成员,通过与胰腺β细胞上的特异性受体结合来刺激胰岛素分泌。此外,GLP-1 通过抑制食欲和延缓胃排空对葡萄糖调节发挥广泛的有益作用。目前,包括艾塞那肽和利拉鲁肽在内的长效 GLP-1 类似物已被批准用于治疗 2 型糖尿病,但长期注射会限制这些慢性患者的使用。在本报告中,作者对非肽类 GLP-1 受体激动剂的开发进行了综述,并介绍了一种新型激动剂 DA-15864。