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 first-in-class inhibitor of protein…
By J. Axten, J. Medina, Yanhong Feng, A. Shu, S. P. Romeril, Seth W. Grant, W. Li, D. Heerding, E. Minthorn, T. Mencken and 14 more. Journal of Medicinal Chemistry, 2012
615 citations recorded by the source corpus.
Subfields: Cell Biology, Epidemiology, Physiology
View Paper: https://www.semanticscholar.org/paper/6ca83a338b34b86381b1ccbc0710809b5120fdd3
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In Cell Biology
- Peter Walter
- J. Cubillos-Ruiz
- Laurie H. Glimcher
- Sarah Bettigole
- D. Ron
- Nahum Sonenberg
- C. Hetz
- Han Li
In Epidemiology
- D. Ron
- Peter Walter
- Laurie H. Glimcher
- J. Cubillos-Ruiz
- Han Li
- Nahum Sonenberg
- Sarah Bettigole
- R. Kaufman
In Physiology
Citations in the corpus
- Pharmacological brake-release of mRNA translation enhances cognitive memory (2013, background): “In agreement, a PERK-specific inhibitor demonstrates antitumor activity in a human pancreatic tumor xenograft model (Axten et al., 2012).”
- ALS/FTD Mutation-Induced Phase Transition of FUS Liquid Droplets and Reversible Hydrogels into Irreversible Hydrogels Impairs RNP Granule Function (2015, background): “We compared the effect of the PERK kinase inhibitor GSK2606414 (Axten et al., 2012) on new protein synthesis in neurons expressing (i) wild-type FUS, (ii) wildtype FUS plus thapsigargin (a well-established activator of the UPR), and (iii) ALS/FTD mutant FUS: FUS(R522G), FUS(R524S), FUS501, or FUS(R4”
- Tumorigenic and Immunosuppressive Effects of Endoplasmic Reticulum Stress in Cancer (2017, positive): “GSK2606414 was the first reported PERK inhibitor (Axten et al., 2012) and was found to be neuroprotective in mouse models of prion disease (Moreno et al., 2013).”