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Protein kinase R-like endoplasmic reticulum kinase (PERK)
- Target
- PERK
- Molecular classification
- Enzyme, Serine/threonine protein kinase, Type I transmembrane protein
01
Overview
Protein kinase R-like endoplasmic reticulum kinase (PERK) is a type I transmembrane serine/threonine protein kinase located in the membrane of the endoplasmic reticulum (ER). It functions as a key sensor and mediator of the unfolded protein response (UPR), which is activated during ER stress caused by accumulation of misfolded proteins. Upon activation, PERK phosphorylates eukaryotic initiation factor 2 alpha (eIF2α), leading to inhibition of general protein synthesis but selective translation of specific mRNAs involved in stress adaptation.
- Other names
- EIF2AK3
02
Mechanism of action
Inhibition of PERK leads to reduced phosphorylation of eIF2α, preventing translational attenuation and downstream effects of the UPR.
03
Biological functions
Unfolded Protein Response (UPR)Integrated Stress ResponseRegulation of mRNA translationApoptosisStress adaptation
04
Disease associations
Wolcott-Rallison syndromeNeurodegenerative diseaseAlzheimer's diseaseSpinal cord injuryDiabetes mellitus
05
Safety considerations
Inhibition of PERK may disrupt the UPR, potentially leading to accumulation of misfolded proteins and cellular dysfunction.
06
Interacting drugs
GSK2606414
2 more in the full profile.
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