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

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Millennium Pharmaceuticals, Inc., 75 Sidney Street, Cambridge, Massachusetts 02139
Cite this: J. Am. Chem. Soc. 2002, 124, 40, 11852–11853
Publication Date (Web):September 12, 2002
https://doi.org/10.1021/ja0277226
Copyright © 2002 American Chemical Society
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    Abstract

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    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.

    †

     Medicinal Chemistry.

    ‡

     Lead Discovery.

    §

     Biochemistry/Enzymology.

    *

     To whom correspondence should be addressed. E-mail:  [email protected].

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