Target intelligence / Profile preview

Endoplasmic reticulum to nucleus signaling 1 (IRE1α)

Target
IRE1α
Molecular classification
Enzyme, Transmembrane protein, Serine/threonine-protein kinase, Endoribonuclease
01

Overview

ERN1/IRE1α is a key sensor of ER stress and a central player in the unfolded protein response (UPR). It possesses both kinase and RNase activity, which are activated upon accumulation of misfolded proteins in the ER. Activated IRE1α splices XBP1 mRNA, leading to the production of XBP1s, a transcription factor that upregulates genes involved in restoring ER homeostasis. Dysregulation of IRE1α is implicated in several diseases, including neurodegenerative disorders and cancer.

Other names
ERN1Inositol-requiring enzyme 1 alphaIRE1IREα
02

Mechanism of action

Kinase and RNase activity regulating the UPR pathway, specifically splicing XBP1 mRNA.

03

Biological functions

Unfolded protein response (UPR)Cellular adaptation to ER stressRegulation of gene expressionER homeostasis
04

Disease associations

Neurodegenerative diseaseAlzheimer's diseaseParkinson's diseaseAmyotrophic lateral sclerosisCancer
05

Safety considerations

Potential for off-target effects due to kinase activity.Dysregulation may lead to ER stress-related pathologies.

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