二肽基肽酶-4抑制剂研究进展  

Advances in Research on Dipeptidyl Peptidase-4 Inhibitors

作　　者：史长丽[1] 葛蔚颖[1] 刘新泳[1] 

机构地区：[1]山东大学药学院药物化学研究所,山东济南250012

出　　处：《药学进展》2012年第8期337-346,共10页Progress in Pharmaceutical Sciences

摘　　要：二肽基肽酶-4抑制剂为一类常用的2型糖尿病治疗药物,可通过抑制二肽基肽酶-4活性延长胰高血糖素样肽-1的作用时间和促进胰岛素分泌,从而降低血糖水平。根据化学结构类型的不同,将二肽基肽酶-4抑制剂分为拟肽类和非拟肽类抑制剂,并分别介绍其药理活性、构效关系及药动学特性等方面的研究进展。Dipeptidyl peptidase-4（DPP-4） inhibitors are a kind of common therapeutic drugs for the treatment of type 2 diabetes.The inhibition of DPP-4 can prolong the action of glucagon-like peptide-1 and improve insulin secretion,so as to lower the glucose level.In this article,the DPP-4 inhibitors were divided into peptidomimetic and non-peptidomimetic inhibitors based on the differences in their chemical structures.Moreover,the advances in research on their pharmacological activities,structure-activity relationships（SARs） and pharmacokinetics were also introduced.

关 键 词：二肽基肽酶-4抑制剂 2型糖尿病 构效关系 

分 类 号：R977.15[医药卫生—药品] R918[医药卫生—药学]