Nature Communications (Nov 2017)

Multicomponent mapping of boron chemotypes furnishes selective enzyme inhibitors

  • Joanne Tan,
  • Armand B. Cognetta III,
  • Diego B. Diaz,
  • Kenneth M. Lum,
  • Shinya Adachi,
  • Soumajit Kundu,
  • Benjamin F. Cravatt,
  • Andrei K. Yudin

DOI
https://doi.org/10.1038/s41467-017-01319-4
Journal volume & issue
Vol. 8, no. 1
pp. 1 – 8

Abstract

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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.