Thiol-based angiotensin-converting enzyme 2 inhibitors: P(1) modifications for the exploration of the S(1) subsite

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Screening of a metalloprotease library led to the identification of a thiol-based dual ACE/NEP inhibitor as a potent ACE2 inhibitor. Modifications of the P(1) benzyl moiety led to improvements in ACE2 potency as well as to increased selectivity versus ACE and NEP.

Detalles Bibliográficos
Autores principales: Deaton, David N., Gao, Enoch N., Graham, Kevin P., Gross, Jeffrey W., Miller, Aaron B., Strelow, John M.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Ltd. Published by Elsevier Ltd. 2008
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7126659/
https://www.ncbi.nlm.nih.gov/pubmed/18078750
http://dx.doi.org/10.1016/j.bmcl.2007.11.048
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author Deaton, David N.
Gao, Enoch N.
Graham, Kevin P.
Gross, Jeffrey W.
Miller, Aaron B.
Strelow, John M.
author_facet Deaton, David N.
Gao, Enoch N.
Graham, Kevin P.
Gross, Jeffrey W.
Miller, Aaron B.
Strelow, John M.
author_sort Deaton, David N.
collection PubMed
description Screening of a metalloprotease library led to the identification of a thiol-based dual ACE/NEP inhibitor as a potent ACE2 inhibitor. Modifications of the P(1) benzyl moiety led to improvements in ACE2 potency as well as to increased selectivity versus ACE and NEP.
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spelling pubmed-71266592020-04-08 Thiol-based angiotensin-converting enzyme 2 inhibitors: P(1) modifications for the exploration of the S(1) subsite Deaton, David N. Gao, Enoch N. Graham, Kevin P. Gross, Jeffrey W. Miller, Aaron B. Strelow, John M. Bioorg Med Chem Lett Article Screening of a metalloprotease library led to the identification of a thiol-based dual ACE/NEP inhibitor as a potent ACE2 inhibitor. Modifications of the P(1) benzyl moiety led to improvements in ACE2 potency as well as to increased selectivity versus ACE and NEP. Elsevier Ltd. Published by Elsevier Ltd. 2008-01-15 2007-11-19 /pmc/articles/PMC7126659/ /pubmed/18078750 http://dx.doi.org/10.1016/j.bmcl.2007.11.048 Text en Copyright © 2007 Elsevier Ltd. Published by Elsevier Ltd. All rights reserved. Since January 2020 Elsevier has created a COVID-19 resource centre with free information in English and Mandarin on the novel coronavirus COVID-19. The COVID-19 resource centre is hosted on Elsevier Connect, the company's public news and information website. Elsevier hereby grants permission to make all its COVID-19-related research that is available on the COVID-19 resource centre - including this research content - immediately available in PubMed Central and other publicly funded repositories, such as the WHO COVID database with rights for unrestricted research re-use and analyses in any form or by any means with acknowledgement of the original source. These permissions are granted for free by Elsevier for as long as the COVID-19 resource centre remains active.
spellingShingle Article
Deaton, David N.
Gao, Enoch N.
Graham, Kevin P.
Gross, Jeffrey W.
Miller, Aaron B.
Strelow, John M.
Thiol-based angiotensin-converting enzyme 2 inhibitors: P(1) modifications for the exploration of the S(1) subsite
title Thiol-based angiotensin-converting enzyme 2 inhibitors: P(1) modifications for the exploration of the S(1) subsite
title_full Thiol-based angiotensin-converting enzyme 2 inhibitors: P(1) modifications for the exploration of the S(1) subsite
title_fullStr Thiol-based angiotensin-converting enzyme 2 inhibitors: P(1) modifications for the exploration of the S(1) subsite
title_full_unstemmed Thiol-based angiotensin-converting enzyme 2 inhibitors: P(1) modifications for the exploration of the S(1) subsite
title_short Thiol-based angiotensin-converting enzyme 2 inhibitors: P(1) modifications for the exploration of the S(1) subsite
title_sort thiol-based angiotensin-converting enzyme 2 inhibitors: p(1) modifications for the exploration of the s(1) subsite
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7126659/
https://www.ncbi.nlm.nih.gov/pubmed/18078750
http://dx.doi.org/10.1016/j.bmcl.2007.11.048
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