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Target intelligence / Profile preview
Glutathione Peroxidase 4 (GPX4)
- Target
- GPX4
- Molecular classification
- Enzyme, Glutathione Peroxidase
01
Overview
Glutathione peroxidase 4 (GPX4) is a selenium-dependent enzyme that protects cells from oxidative damage by reducing lipid hydroperoxides within biological membranes. It is a central regulator of ferroptosis, a form of iron-dependent cell death, and its inactivation leads to the accumulation of toxic lipid peroxides. GPX4 plays roles in inflammation resolution and eicosanoid biosynthesis. It has emerged as an important pharmacological target, with inhibitors being investigated for their ability to induce ferroptosis in therapy-resistant cancer cells.
02
Mechanism of action
GPX4 inhibitors induce ferroptosis by preventing the reduction of lipid hydroperoxides, leading to their accumulation and subsequent cell death.
03
Biological functions
Antioxidant defenseProtection against oxidative stressRegulation of ferroptosisInflammation resolutionEicosanoid biosynthesisCytokine signaling regulation
04
Disease associations
Spondylometaphyseal dysplasiaCancerNeurodegenerative disease (potential)Oxidative stress related diseases
05
Safety considerations
Off-target effects of GPX4 inhibitorsPotential for inducing ferroptosis in healthy cellsContext-dependent effects (neuroprotection vs. anti-cancer)Complex role in inflammation
06
Interacting drugs
GPX4 inhibitors (e.g., RSL3, ML210)
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