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

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

  • J Am Chem Soc. 2002 Oct 9;124(40):11852-3. doi: 10.1021/ja0277226.
Natalie A Dales 1 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
Affiliations

Affiliation

  • 1 Millennium Pharmaceuticals, Inc., 75 Sidney Street, Cambridge, MA 02139, USA.
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.

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