Discovery of 7-Methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a Potent and Selective …
JM Axten, JR Medina, Y Feng, A Shu… - Journal of medicinal …, 2012 - ACS Publications
JM Axten, JR Medina, Y Feng, A Shu, SP Romeril, SW Grant, WHH Li, DA Heerding…
Journal of medicinal chemistry, 2012•ACS PublicationsProtein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) is activated in response
to a variety of endoplasmic reticulum stresses implicated in numerous disease states.
Evidence that PERK is implicated in tumorigenesis and cancer cell survival stimulated our
search for small molecule inhibitors. Through screening and lead optimization using the
human PERK crystal structure, we discovered compound 38 (GSK2606414), an orally
available, potent, and selective PERK inhibitor. Compound 38 inhibits PERK activation in …
to a variety of endoplasmic reticulum stresses implicated in numerous disease states.
Evidence that PERK is implicated in tumorigenesis and cancer cell survival stimulated our
search for small molecule inhibitors. Through screening and lead optimization using the
human PERK crystal structure, we discovered compound 38 (GSK2606414), an orally
available, potent, and selective PERK inhibitor. Compound 38 inhibits PERK activation in …
Protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states. Evidence that PERK is implicated in tumorigenesis and cancer cell survival stimulated our search for small molecule inhibitors. Through screening and lead optimization using the human PERK crystal structure, we discovered compound 38 (GSK2606414), an orally available, potent, and selective PERK inhibitor. Compound 38 inhibits PERK activation in cells and inhibits the growth of a human tumor xenograft in mice.
ACS Publications