PERK

PERK

Protein kinase RNA-like endoplasmic reticulum kinase (PERK; EC 2.7.11.1) is a type I ER membrane protein and one of three (next to IRE1 and ATF6) primary effectors of the unfolded protein response (UPR), which has a demonstrated role in tumor growth and angiogenesis. Increase in unfolded proteins in the ER causes release of ER chaperones from the stress-sensing domain of PERK, which results in its activation via oligomerization and autophosphorylation at multiple serine, threonine, and tyrosine residues. Upon activation, PERK phosphorylates eukaryotic initiation factor 2α (eIF2α), rendering it an inhibitor of the ribosome translation initiation complex, consequently reducing overall protein synthesis. The reduction in translation reduces the ER burden, providing time for the cell to process or degrade the accumulated unfolded proteins to restore ER homeostasis.

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  • GSK 2606414
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    GSK 2606414
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    2278
    ISRIB
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More About PERK

Protein kinase RNA-like endoplasmic reticulum kinase (PERK; EC 2.7.11.1) is a type I ER membrane protein and one of three (next to IRE1 and ATF6) primary effectors of the unfolded protein response (UPR), which has a demonstrated role in tumor growth and angiogenesis. Increase in unfolded proteins in the ER causes release of ER chaperones from the stress-sensing domain of PERK, which results in its activation via oligomerization and autophosphorylation at multiple serine, threonine, and tyrosine residues. Upon activation, PERK phosphorylates eukaryotic initiation factor 2α (eIF2α), rendering it an inhibitor of the ribosome translation initiation complex, consequently reducing overall protein synthesis. The reduction in translation reduces the ER burden, providing time for the cell to process or degrade the accumulated unfolded proteins to restore ER homeostasis[1].

[1] J.M. Axten et al. 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 kinase R (PKR)-like endoplasmic reticulum kinase (PERK). J. Med. Chem. 2012, 55, 7193-7207.

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