二肽基肽酶-4及其抑制剂的研究进展

王欣,李游,桂辛蕊,程先超

中国药学杂志 ›› 2013, Vol. 48 ›› Issue (21) : 1789-1796.

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中国药学杂志 ›› 2013, Vol. 48 ›› Issue (21) : 1789-1796. DOI: 10.11669/cpj.2013.21.003
综述

二肽基肽酶-4及其抑制剂的研究进展

  • 王欣1, 李游2,桂辛蕊2,程先超2,*
作者信息 +

Progress in Dipeptidyl Peptidase-4 and Its Inhibitors

  • WANG Xin1, LI You2, GUI Xin-rui2, CHENG Xian-chao2,*
Author information +
文章历史 +

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。

Abstract

To review the structures of dipeptidyl peptidase-4(DPP-4)and its inhibitors and introduce the evaluation 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 phases. The structure-activity relationship study of various reported inhibitors could promote the development of more efficient DPP-4 inhibitors.

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

Key words

DPP-4 / DPP-4 inhibitor / type 2 diabetes / structure-activity relationship

引用本文

导出引用
王欣,李游,桂辛蕊,程先超. 二肽基肽酶-4及其抑制剂的研究进展[J]. 中国药学杂志, 2013, 48(21): 1789-1796 https://doi.org/10.11669/cpj.2013.21.003
WANG Xin, LI You, GUI Xin-rui,CHENG Xian-chao. Progress in Dipeptidyl Peptidase-4 and Its Inhibitors[J]. Chinese Pharmaceutical Journal, 2013, 48(21): 1789-1796 https://doi.org/10.11669/cpj.2013.21.003
中图分类号: R944   

参考文献

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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)

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