Development of potent and selective dipeptidyl peptidase II inhibitors

被引：32
|
作者：
Senten, K
Van der Veken, P
Bal, G
De Meester, I
Lambeir, AM
Scharpé, S
Bauvois, B
Haemers, A
Augustyns, K
机构：
[1] Univ Antwerp UIA, Dept Med Chem, B-2610 Wilrijk, Belgium
[2] Inst Curie, INSERM, U365, F-75231 Paris 05, France
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 20期
关键词：
D O I：
10.1016/S0960-894X(02)00603-0
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Structure-activity investigations of product-like dipeptide analogues lacking the C-terminal carbonyl function resulted in potent and selective dipeptidyl peptidase II (DPP II) inhibitors. Dab-Pip has an IC50 = 0.13 muM for DPP II and a 7600-fold selectivity with respect to DPP IV. This compound will be highly valuable for the investigation of the biochemical function of DPP II. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：2825 / 2828
页数：4
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