Discovery of 1H-Pyrazol-3(2H)-ones as Potent and Selective Inhibitors of Protein Kinase R-like Endoplasmic Reticulum Kinase (PERK)

Autor:	David Powers, Katja Labitzke, Mark J. Rose, Kristin L. Andrews, Richard Kendall, Kenneth R. Dellamaggiore, Shon Booker, Peter Jaeckel, Silvia Materna-Reichelt, Mark H. Norman, Young-Ah Chung, Holger Beckmann, Paul L. Shaffer, Pedro J. Beltran, Hao Chen, Alexander M. Long, Petia Mitchell, Adrian L. Smith, Jennifer Dao, J. Russell Lipford, Noel D'angelo, Steven F. Bellon, Michelle Wu
Rok vydání:	2015
Předmět:	Models Molecular endocrine system Dose-Response Relationship Drug Molecular Structure Kinase Drug discovery Chemistry Endoplasmic reticulum Mice Nude Protein kinase R In vitro Mice Structure-Activity Relationship eIF-2 Kinase Biochemistry In vivo Drug Discovery Animals Humans Pyrazoles Molecular Medicine Structure–activity relationship PERK inhibitors Protein Kinase Inhibitors Cells Cultured
Zdroj:	Journal of Medicinal Chemistry. 58:1426-1441
ISSN:	1520-4804 0022-2623
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::906c5b60a94b9bc681eaaf3c8dfd6af5 https://doi.org/10.1021/jm5017494 Zobrazit plný text záznamu