Target intelligence / Profile preview

Kelch-like ECH-associated protein 1–nuclear factor erythroid 2-related factor 2 pathway (KEAP1-Nrf2)

Target: KEAP1-Nrf2
Molecular classification: Signaling Pathway, Transcription factor regulator, Protein-protein interaction

Overview

The KEAP1-Nrf2 pathway is a critical cellular defense mechanism against oxidative and electrophilic stress. Under basal conditions, KEAP1 targets Nrf2 for degradation. Upon exposure to stress, KEAP1 releases Nrf2, allowing it to translocate to the nucleus, bind ARE elements, and activate the expression of genes involved in antioxidant defense, detoxification, and cellular protection.

Other names: Nrf2 pathwayNFE2L2 pathwayAntioxidant Response Element pathwayARE pathwayKeap1-Nrf2 signaling pathway

Mechanism of action

Modulation of KEAP1-Nrf2 interaction, leading to Nrf2 stabilization, nuclear translocation, and activation of ARE-dependent gene expression.

Biological functions

Antioxidant defenseDetoxificationRedox homeostasisStress responseGene regulationCell survival

Disease associations

CancerInflammationNeurodegenerative diseaseCardiovascular diseaseAgingMetabolic disorders

Safety considerations

Off-target effects of Nrf2 activatorsPotential for tumor promotion with sustained Nrf2 activationChemoresistance development in cancerDrug-drug interactions

Interacting drugs

Sulforaphane

4 more in the full profile.

Biomarkers

Nrf2 expression levelsKEAP1 mutation statusARE-dependent gene expression (e.g., HO-1, NQO1)Oxidative stress markers (e.g., ROS levels)

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