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Glutathione S-Transferases (GSTs) are members of the phase II detoxification enzyme family that conjugate glutathione to various electrophilic compounds, including metabolites generated by oxidative processes in the body, environmental toxins or carcinogens, and anti-cancer drugs. GSTP1 is a cytosolic protein that belongs to pi class of the GST superfamily. It is crystallized as a homodimer, but also exists in solution as an equilibrium mixture of monomer and dimer, depending on the protein concentration. Human GSTP1 is present at elevated levels in many tumor cells, and has unique properties as a cancer marker. Genetic polymorphisms and expression patterns of GSTP1 have been associated with a variety of effects on human cancer, anti-cancer drug resistance, and asthma. In addition to its role as a drug-metabolizing enzyme, GSTP1 has ligand binding properties and regulates kinase signaling pathways through protein-protein interactions.