Drug pipeline
Full profile accessExplore the programs pursuing this target and their development progress.
- Drug candidates
- Developers
- Development stage
Target intelligence / Profile preview
Eukaryotic translation initiation factor 2 alpha kinase PERK (PERK)
- Target
- PERK
- Molecular classification
- Enzyme, Protein Kinase, Serine/Threonine Kinase, Type I transmembrane protein
01
Overview
PERK (Eukaryotic translation initiation factor 2 alpha kinase PERK) is a type I transmembrane serine/threonine protein kinase located in the endoplasmic reticulum (ER) membrane. It functions as a key sensor and mediator of the unfolded protein response (UPR), activated by ER stress due to the accumulation of misfolded proteins. Upon activation, PERK phosphorylates eIF2α, inhibiting general mRNA translation, but selectively allowing translation of UPR-related transcripts like ATF4. Mutations in PERK cause Wolcott-Rallison syndrome. PERK interacts with proteins like DNAJC3, NFE2L2, and BiP/Grp78. Small molecule inhibitors like GSK2606414 are used to study PERK function.
- Other names
- Protein kinase R (PKR)-like endoplasmic reticulum kinaseEIF2AK3
02
Mechanism of action
Inhibition of PERK kinase activity, leading to modulation of the UPR and downstream signaling pathways.
03
Biological functions
Unfolded protein response (UPR)ER stress sensingRegulation of protein synthesiseIF2α phosphorylationApoptosisBone homeostasis
04
Disease associations
Wolcott-Rallison syndromeDiabetes mellitusSkeletal dysplasiaDiseases linked to proteostasis imbalance
05
Safety considerations
Potential for off-target effects due to kinase family similaritiesDisruption of cellular homeostasis by complete UPR inhibitionPotential for promoting or inhibiting apoptosis depending on context
06
Interacting drugs
GSK2606414
1 more in the full profile.
Beyond the preview
Go deeper on Eukaryotic translation initiation factor 2 alpha kinase PERK (PERK).
Explore the evidence, development activity, and competitive landscape with Gosset’s full data platform.
Clinical trials
Full profile accessFollow the clinical studies evaluating therapies directed at this target.
- Trial design
- Status
- Readouts
Competitive landscape
Full profile accessCompare approaches across drug candidates, modalities, and indications.
- Programs
- Modalities
- Indications
Literature & evidence
Full profile accessInvestigate the research and source evidence behind target biology and development.
- Publications
- Sources
- Analysis
Patents
Full profile accessExplore patent activity around therapies and technologies addressing this target.
- Patents
- Assignees
- Technologies
Research & analysis
Full profile accessConnect target biology, drug development, and emerging evidence in your research.
- Biology
- Development news
- Analysis
Bring the full picture into focus.
See how Gosset can support your research on Eukaryotic translation initiation factor 2 alpha kinase PERK (PERK).