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Eukaryotic translation initiation factor 2a kinase 3 (EIF2AK3; PERK)

Mouse studies suggest inhibiting PERK could help treat prion-associated diseases. Misfolded prion proteins in the brain activate PERK to trigger the unfolded protein response, which shuts down the normal translation process required for neuron function and survival. In mice infected with prions, the oral PERK inhibitor GSK2606414 prevented further neurodegeneration and the associated behavioral and memory symptoms. In the brains of treated mice, normal protein translation was restored. Next steps could include testing PERK inhibitors in additional models of prion-associated diseases.
GlaxoSmithKline plc collaborated on the study. The pharma has no disclosed PERK inhibitors in development.
GSK2606414 is a research reagent.

SciBX 6(43); doi:10.1038/scibx.2013.1232
Published online Nov. 7, 2013

Patent application filed by GlaxoSmithKline covering GSK2606414 and other PERK inhibitors; licensing status unavailable

Moreno, J.A. et al. Sci. Transl. Med.; published online Oct. 9, 2013;
Contact: Giovanna R. Mallucci, University of Leicester, Leicester, U.K.