中文摘要：

目的简述二肽基肽酶4（DPP4）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。

英文摘要：

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.