1区 · 医学
Article
作者: Rose, Mark ; Andrews, Kristin L. ; Wu, Michelle M. ; Beltran, Pedro J. ; Booker, Shon ; Materna-Reichelt, Silvia ; Labitzke, Katja ; Jaeckel, Peter ; Kendall, Richard ; Dao, Jennifer ; Shaffer, Paul L. ; Bellon, Steven F. ; Beckmann, Holger ; Smith, Adrian L. ; Lipford, J. Russell ; D'Angelo, Noel D. ; Dellamaggiore, Kenneth R. ; Chung, Young-Ah ; Mitchell, Petia ; Chen, Hao ; Long, Alexander M. ; Powers, David ; Norman, Mark H.
The structure-based design and optimization of a novel series of selective PERK inhibitors are described resulting in the identification of 44 as a potent, highly selective, and orally active tool compound suitable for PERK pathway biology exploration both in vitro and in vivo.