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Target intelligence / Profile preview
Glutathione S-transferase P1-1 (GSTP1-1)
- Target
- GSTP1-1
- Molecular classification
- Enzyme, Transferase
01
Overview
Glutathione S-transferase P1-1 (GSTP1-1) is a phase II detoxification enzyme that catalyzes the conjugation of glutathione to various hydrophobic and electrophilic compounds, playing a critical role in cellular defense against oxidative stress and toxic insults. It is a homodimer with two subunits, each containing a glutathione-binding site (G-site) and a hydrophobic substrate-binding site (H-site). Genetic polymorphisms, particularly at residue 105, affect substrate specificity and stability. GSTP1-1 is overexpressed in various cancers, contributing to drug resistance. Inhibitors are being developed to overcome chemoresistance in cancer therapies.
02
Mechanism of action
Inhibition of glutathione conjugation
03
Biological functions
DetoxificationXenobiotic metabolismAntioxidant defenseLigandin activity
04
Disease associations
CancerDrug resistanceAsthma
05
Safety considerations
Inhibition may disrupt normal detoxification processesGenetic polymorphisms may influence drug response
06
Interacting drugs
Ethacrynic acid
1 more in the full profile.
07
Biomarkers
GSTP1-1 overexpression (cancer marker)
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