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9451 13666 Ensembl ENSG00000172071 ENSMUSG00000031668 UniProt Q9NZJ5 Q9Z2B5 RefSeq (mRNA) NM_001313915 NM_004836 NM_010121 NM_001313918 RefSeq (protein) NP_001300844 NP_004827 NP_001300847 NP_034251 Location (UCSC) Chr 2: 88.56 – 88.69 Mb Chr 6: 70.82 – 70.88 Mb PubMed search Wikidata View/Edit Human View/Edit Mouse Eukaryotic translation initiation factor 2-alpha kinase 3, also known as ...
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GSK2606414 was found to be a potent and selective inhibitor of PERK, with good oral bioavailability and blood-brain barrier penetration. [1] PERK mediates the unfolded protein response pathway which is involved in the initiation of protein synthesis, and this pathway has been implicated in the neurotoxicity of various diseases including prion ...
The activated PERK kinase will then phosphorylate eIF2α, causing a cascade of events. Thus, the activation of this kinase is dependent on the aggregation of unfolded proteins in the endoplasmic reticulum. PERK has also been observed to activate in response to activity of the proto-oncogene MYC.
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A PERK inhibitor is a small molecule compound that unlike any existing drug inhibits the expression of protein kinase RNA–like endoplasmic reticulum kinase. The (first such) inhibitor demonstrated the ability to halt brain cell death in mice with prion disease .