Multicomponent mapping of boron chemotypes furnishes selective enzyme inhibitors
oleh: Joanne Tan, Armand B. Cognetta III, Diego B. Diaz, Kenneth M. Lum, Shinya Adachi, Soumajit Kundu, Benjamin F. Cravatt, Andrei K. Yudin
| Format: | Article |
|---|---|
| Diterbitkan: | Nature Portfolio 2017-11-01 |
Deskripsi
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.