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Target intelligence / Profile preview
Unfolded Protein Response (UPR) pathway (UPR)
- Target
- UPR
- Molecular classification
- Other (cellular stress response pathway)
01
Overview
The Unfolded Protein Response (UPR) is a cellular stress response pathway activated by the accumulation of misfolded proteins in the endoplasmic reticulum (ER). It aims to restore ER homeostasis by reducing protein translation, enhancing protein folding, and promoting the degradation of misfolded proteins. The UPR is mediated by three main branches: PERK, IRE1α, and ATF6. It plays a crucial role in various diseases, including cancer, neurodegenerative disorders, and diabetes.
- Other names
- Endoplasmic reticulum stress pathwayER stress response
02
Mechanism of action
Drugs targeting the UPR typically work by modulating the activity of the three main branches of the UPR (PERK, IRE1α, and ATF6) to either alleviate ER stress or induce apoptosis in cancer cells.
03
Biological functions
Signal transductionApoptosisCell deathAutophagyProtein synthesis regulationER-associated degradation (ERAD)
04
Disease associations
Neurodegenerative diseasesCancerInflammationCardiovascular diseaseDiabetes
05
Safety considerations
The primary safety concern is the potential for prolonged ER stress to lead to cell death, which can be beneficial in cancer treatment but harmful in other contexts.
06
Interacting drugs
Various drugs targeting the UPR components, such as PERK inhibitors or IRE1α inhibitors, are under investigation.
07
Biomarkers
GRP78CHOPXBP1ATF4
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