Substrate-Based Design of the First Class of Angiotensin-Converting Enzyme-Related Carboxypeptidase (ACE2) Inhibitors

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• 作者：Natalie A. Dales ; Alexandra E. Gould ; James A. Brown ; Emily F. Calderwood ; Bing Guan ; Charles A. Minor ; James M. Gavin ; Paul Hales ; Virendar K. Kaushik ; Michael Stewart ; Peter J. Tummino ; Chad S. Vick
• 刊名：Journal of the American Chemical Society
• 出版年：2002
• 出版时间：October 9, 2002
• 年：2002
• 卷：124
• 期：40
• 页码：11852 - 11853
• 全文大小：47K
• 年卷期：v.124,no.40(October 9, 2002)
• ISSN：1520-5126

文摘

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.