- Discovery of 1H-pyrazol-3(2H)-ones as potent and selective inhibitors of protein kinase R-like endoplasmic reticulum kinase (PERK).
Discovery of 1H-pyrazol-3(2H)-ones as potent and selective inhibitors of protein kinase R-like endoplasmic reticulum kinase (PERK).
Journal of medicinal chemistry (2015-01-15)
Adrian L Smith, Kristin L Andrews, Holger Beckmann, Steven F Bellon, Pedro J Beltran, Shon Booker, Hao Chen, Young-Ah Chung, Noel D D'Angelo, Jennifer Dao, Kenneth R Dellamaggiore, Peter Jaeckel, Richard Kendall, Katja Labitzke, Alexander M Long, Silvia Materna-Reichelt, Petia Mitchell, Mark H Norman, David Powers, Mark Rose, Paul L Shaffer, Michelle M Wu, J Russell Lipford
PMID25587754
RÉSUMÉ
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.
MATÉRIAUX