Inhibitors of proline-specific a dipeptidyl peptidases: DPP IV inhibitors as a novel approach for the treatment of Type 2 diabetes

被引：41

作者：

Augustyns, K ^{[1
]}

Van der Veken, P ^{[1
]}

Haemers, A ^{[1
]}

机构：

[1] Univ Instelling Antwerp, Dept Med Chem, B-2610 Antwerp, Belgium

来源：

EXPERT OPINION ON THERAPEUTIC PATENTS | 2005年 / 15卷 / 10期

关键词：

dipeptidyl peptidase IV (DPP IV); DPPII; DPP8; DPP9; FAP alpha; medicinal chemistry; Type; 2; diabetes;

D O I：

10.1517/13543776.15.10.1387

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Dipeptidyl peptidase IV (DPP IV) is a validated target for the treatment of Type 2 diabetes, with several inhibitors currently in Phase III clinical trials. This review will mainly focus on DPP IV inhibitors that were published in scientific literature and patents after 2002. Medicinal chemistry aspects of several classes of inhibitors are described with respect to inhibitory potency, selectivity over DPP8, DPP9, FAP alpha and DPP II, stability and ADME/Tox issues. Although the main part of this review is on potent and selective DPP IV inhibitors, selective inhibitors for the related proline-specific dipeptidyl peptidases will be described.

引用

页码：1387 / 1407

页数：21

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