Substrate-based design of the first class of angiotensin-converting enzyme-related carboxypeptidase (ACE2) inhibitors

被引：154

作者：

Dales, NA

Gould, AE

Brown, JA

Calderwood, EF

Guan, B

Minor, CA

Gavin, JM

Hales, P

Kaushik, VK

Stewart, M

Tummino, PJ

Vickers, CS

Ocain, TD

Patane, MA

机构：

[1] Millennium Pharmaceut Inc, Med Chem, Cambridge, MA 02139 USA

[2] Millennium Pharmaceut Inc, Lead Discovery, Cambridge, MA 02139 USA

[3] Millennium Pharmaceut Inc, Biochem Enzymol, Cambridge, MA 02139 USA

来源：

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY | 2002年 / 124卷 / 40期

关键词：

D O I：

10.1021/ja0277226

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Angiotensin-converting enzyme-related carboxypeptidase (ACE2) is a recently identified zinc metalloprotease with carboxypeptidase activity that was identified using our genomics platform. We implemented a rational design approach to identify potent and selective ACE2 inhibitors. To this end, picomolar inhibitors of ACE2 were designed and synthesized. Copyright © 2002 American Chemical Society.

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页码：11852 / 11853

页数：2

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