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