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Substrate-based design of the first class of angiotensin-converting enzyme-related carboxypeptidase (ACE2) inhibitors |
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| Authors: | Dales Natalie A Gould Alexandra E Brown James A Calderwood Emily F Guan Bing Minor Charles A Gavin James M Hales Paul Kaushik Virendar K Stewart Michael Tummino Peter J Vickers Chad S Ocain Timothy D Patane Michael A |
| Affiliation: | 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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