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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Nature Portfolio
2017
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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) |
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DOAJ |
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Science Q |
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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 |
work_keys_str_mv |
AT joannetan multicomponentmappingofboronchemotypesfurnishesselectiveenzymeinhibitors AT armandbcognettaiii multicomponentmappingofboronchemotypesfurnishesselectiveenzymeinhibitors AT diegobdiaz multicomponentmappingofboronchemotypesfurnishesselectiveenzymeinhibitors AT kennethmlum multicomponentmappingofboronchemotypesfurnishesselectiveenzymeinhibitors AT shinyaadachi multicomponentmappingofboronchemotypesfurnishesselectiveenzymeinhibitors AT soumajitkundu multicomponentmappingofboronchemotypesfurnishesselectiveenzymeinhibitors AT benjaminfcravatt multicomponentmappingofboronchemotypesfurnishesselectiveenzymeinhibitors AT andreikyudin multicomponentmappingofboronchemotypesfurnishesselectiveenzymeinhibitors |
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1718385978922500096 |