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Discovery of 2-amino-3-amido-5-aryl-pyridines as highly potent, orally bioavailable, and efficacious

Journal Article · · Bioorg. Med. Chem. Lett.
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Research Organization:
Advanced Photon Source (APS), Argonne National Laboratory (ANL), Argonne, IL (US)
Sponsoring Organization:
DOE - Office Of Science; NIH
OSTI ID:
1836760
Journal Information:
Bioorg. Med. Chem. Lett., Journal Name: Bioorg. Med. Chem. Lett. Vol. 43
Country of Publication:
United States
Language:
ENGLISH

References (15)

Protein kinase R(PKR)–like endoplasmic reticulum kinase (PERK) inhibitors: a patent review (2010-2015) journal September 2016
The Unfolded Protein Response and Cell Fate Control journal January 2018
Endoplasmic Reticulum Stress and the Hallmarks of Cancer journal May 2016
Protein translation and folding are coupled by an endoplasmic-reticulum-resident kinase journal January 1999
Identification and Characterization of Pancreatic Eukaryotic Initiation Factor 2 α-Subunit Kinase, PEK, Involved in Translational Control journal December 1998
VHL Inactivation in Precancerous Kidney Cells Induces an Inflammatory Response via ER Stress–Activated IRE1 α Signaling journal May 2017
Classification of small molecule protein kinase inhibitors based upon the structures of their drug-enzyme complexes journal January 2016
Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development journal August 2013
Activation-dependent substrate recruitment by the eukaryotic translation initiation factor 2 kinase PERK journal January 2006
Discovery of 1 H -Pyrazol-3(2 H )-ones as Potent and Selective Inhibitors of Protein Kinase R-like Endoplasmic Reticulum Kinase (PERK) journal January 2015
When PERK inhibitors turn out to be new potent RIPK1 inhibitors: critical issues on the specificity and use of GSK2606414 and GSK2656157 journal April 2017
When ER stress reaches a dead end journal December 2013
Discovery of 7-Methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1 H -indol-5-yl)-7 H -pyrrolo[2,3- d ]pyrimidin-4-amine (GSK2606414), a Potent and Selective First-in-Class Inhibitor of Protein Kinase R (PKR)-like Endoplasmic Reticulum Kinase (PERK) journal August 2012
The Unfolded Protein Response: From Stress Pathway to Homeostatic Regulation journal November 2011
Signal integration in the endoplasmic reticulum unfolded protein response journal July 2007

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