Journal of the American Chemical Society 2002-10-09

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

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 Vickers, Timothy D Ocain, Michael A Patane

Index: J. Am. Chem. Soc. 124(40) , 11852-3, (2002)

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Abstract

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.