Multicomponent mapping of boron chemotypes furnishes selective enzyme inhibitors

Heteroatom-rich organoboron compounds are promising modulators of enzyme activity. Here, the authors report a library of aminocyanoboronates as serine hydrolases inhibitors with the most potent compound showing in vivo and in vitro nanomolar activity and high selectivity towards human ABHD3 hydrolas...

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Autores principales: Joanne Tan, Armand B. Cognetta III, Diego B. Diaz, Kenneth M. Lum, Shinya Adachi, Soumajit Kundu, Benjamin F. Cravatt, Andrei K. Yudin
Formato: article
Lenguaje:EN
Publicado: Nature Portfolio 2017
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Acceso en línea:https://doaj.org/article/2aff97f7effa472ca74895e649dd461a
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spelling oai:doaj.org-article:2aff97f7effa472ca74895e649dd461a2021-12-02T15:38:58ZMulticomponent mapping of boron chemotypes furnishes selective enzyme inhibitors10.1038/s41467-017-01319-42041-1723https://doaj.org/article/2aff97f7effa472ca74895e649dd461a2017-11-01T00:00:00Zhttps://doi.org/10.1038/s41467-017-01319-4https://doaj.org/toc/2041-1723Heteroatom-rich organoboron compounds are promising modulators of enzyme activity. Here, the authors report a library of aminocyanoboronates as serine hydrolases inhibitors with the most potent compound showing in vivo and in vitro nanomolar activity and high selectivity towards human ABHD3 hydrolase.Joanne TanArmand B. Cognetta IIIDiego B. DiazKenneth M. LumShinya AdachiSoumajit KunduBenjamin F. CravattAndrei K. YudinNature PortfolioarticleScienceQENNature Communications, Vol 8, Iss 1, Pp 1-8 (2017)
institution DOAJ
collection DOAJ
language EN
topic Science
Q
spellingShingle Science
Q
Joanne Tan
Armand B. Cognetta III
Diego B. Diaz
Kenneth M. Lum
Shinya Adachi
Soumajit Kundu
Benjamin F. Cravatt
Andrei K. Yudin
Multicomponent mapping of boron chemotypes furnishes selective enzyme inhibitors
description Heteroatom-rich organoboron compounds are promising modulators of enzyme activity. Here, the authors report a library of aminocyanoboronates as serine hydrolases inhibitors with the most potent compound showing in vivo and in vitro nanomolar activity and high selectivity towards human ABHD3 hydrolase.
format article
author Joanne Tan
Armand B. Cognetta III
Diego B. Diaz
Kenneth M. Lum
Shinya Adachi
Soumajit Kundu
Benjamin F. Cravatt
Andrei K. Yudin
author_facet Joanne Tan
Armand B. Cognetta III
Diego B. Diaz
Kenneth M. Lum
Shinya Adachi
Soumajit Kundu
Benjamin F. Cravatt
Andrei K. Yudin
author_sort Joanne Tan
title Multicomponent mapping of boron chemotypes furnishes selective enzyme inhibitors
title_short Multicomponent mapping of boron chemotypes furnishes selective enzyme inhibitors
title_full Multicomponent mapping of boron chemotypes furnishes selective enzyme inhibitors
title_fullStr Multicomponent mapping of boron chemotypes furnishes selective enzyme inhibitors
title_full_unstemmed Multicomponent mapping of boron chemotypes furnishes selective enzyme inhibitors
title_sort multicomponent mapping of boron chemotypes furnishes selective enzyme inhibitors
publisher Nature Portfolio
publishDate 2017
url https://doaj.org/article/2aff97f7effa472ca74895e649dd461a
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