二肽基肽酶-4及其抑制剂的研究进展  

Progress in Dipeptidyl Peptidase-4 and Its Inhibitors

作　　者：王欣[1] 李游[2] 桂辛蕊[2] 程先超[2] 

机构地区：[1]天津生物工程职业技术学院,天津300462 [2]天津市临床药物关键技术重点实验室,天津医科大学药学院,天津300070

出　　处：《中国药学杂志》2013年第21期1789-1796,共8页Chinese Pharmaceutical Journal

基　　金：国家自然科学基金资助项目(21202120);中国博士后科学基金(2012T50237;20100480655);天津医科大学"新世纪优秀人才"基金;天津市高等学校科技发展基金(20100101)

摘　　要：目的简述二肽基肽酶-4(DPP-4)的结构及功能,根据二肽基肽酶-4抑制剂的结构特点对其进行分类介绍,并结合已上市的二肽基肽酶-4抑制剂介绍其活性评价方法。方法查阅国内外相关文献并进行归纳、分析综述。结果与结论二肽基肽酶-4作为经临床证实的治疗2型糖尿病的新靶点,近年来引起医药界的广泛关注,越来越多的候选药物进入各期临床研究中,总结各类抑制剂的构效关系为更加高效的抑制剂的开发奠定坚实的基础。OBJECTIVE To review the structures of dipeptidyl peptidase-4 （DPP-4） and its inhibitors and introduce the evalua- tion methods of several marketed inhibitors. METHODS Preparation of this review is based on searching, categorizing, analyzing and summarizing of diplomatic and international literatures about DPP-4 and its inhibitors. RESULTS AND CONCLUSION DPP-4 has attracted a lot of attention as a new target of type 2 diabetes, and some drug candidates have been developed and entered clinical pha- ses. The structure-activity relationship study of various reported inhibitors could promote the development of more efficient DPP-4 inhib- itors.

关 键 词：二肽基肽酶-4 二肽基肽酶4抑制剂 2型糖尿病 构效关系 

分 类 号：R944[医药卫生—药剂学]