胰高血糖素样肽-1受体激动剂的研究进展

作者:王晶;曲本龙;祁亦男;陈建超;孙铁民; 刊名:中南药学 上传者:王晓卫

【摘要】在健康人中,肠降血糖素胰高血糖素样肽-1(GLP-1)是在进食后分泌,并通过增加胰岛素分泌和抑制胰高血糖素释放而降低葡萄糖浓度。天然GLP-1在体内降解时间约为2~3 min,因此需要开发各种GLP-1受体激动剂以延长其体内作用时间。已开发出的GLP-1受体激动剂分为短期受体激活的化合物(例如艾塞那肽)和GLP-1受体的长效化合物(例如阿必鲁肽和利拉鲁肽等),以及小分子非肽类药物。这些GLP-1受体激动剂的个体性质可能使基于肠降血糖素的2型糖尿病治疗满足每个患者的需要。本文对当前GLP-1激动剂类药物的研究进行了综述。

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553 中南药学 2017 年 5 月 第 15 卷 第 5 期 Central South Pharmacy. May 2017, Vol. 15 No.5 ma-(4-Aryl-1-piperazinyl)-l-prolyl] thiazolidines as a novel series of highly potent and long-lasting DPP-Ⅳ in-hibitors [J]. Bioorg Med Chem Lett,2007,17(9):2618- 2621. [32] Forst T,Uhliglaske B,Ring A,et al. Linagliptin(BI 1356), a potent and selective DPP-4 inhibitor,is safe and efficacious in combination with metformin in patients with inadequately controlled type 2 diabetes [J]. Diabetic Med,2010,27(12): 1409-1419. [33] Chyan YJ,Chuang LM. Dipeptidyl peptidase-Ⅳ inhib-itors:An evolving treatment for type 2 diabetes from the incretin concept [J]. Recent Pat Endocr Metab Immune Drug Discov,2007,1(1): 15-24. [34] Pei Z,Li X,von Geldern TW,et al. Discovery and structure-activity relationships of piperidinone and piperidine-constrained phenethylamines as novel,po-tent,and selective dipeptidyl peptidase Ⅳ inhibitors [J]. J Med Chem,2007,50(8): 1983-1987. [35] Cox JM,Edmondson SD,Harper B,et al. Aminopiperi-dines as dipeptidyl peptidase-Ⅳ inhibitors for the treatment or prevention of diabetes:U. S. Patent 7,884,104[P]. 2011-02-08. [36] Kim HJ,Kwak WY,Min JP,et al. Discovery of DA- 1229:a potent,long acting dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes [J]. Bioorg Med Chem Lett,2011,21(12): 3809-3812. [37] Biftu T,Sinha-Roy R,Chen P,et al. Omarigliptin(MK-3102):a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. [J]. J Med Chem,2014,57 (8): 3205-32

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