グルタチオンSトランスフェラーゼ (GST) 阻害剤
Glutathione S-transferases (GSTs) constitute a family of phase II detoxification isozymes that catalyze the conjugation of glutathione with a number of hydrophobic compounds. Due to high expression of GSTs in tumors compared to normal tissues and their high level in plasma from cancer patients, these enzymes are considered to be cancer markers. All species possess multiple cytosolic and membrane-bound GST isozymes. These isozymes differ in their tissue-specific expression and distribution. They provide protection to mammalian cells against the toxic and neoplastic effects of electrophilic metabolites of carcinogens and reactive oxygen species. Increased expression of GST isozymes has been linked to the development of resistance to alkylating cytostatic drugs. Their deficiency reportedly increases predisposition to various forms of cancer. Hence, GST status may be a useful prognostic factor to determine the clinical outcome of chemotherapy.
References:
Wu, Z., et al. 2004. J. Med. Chem. 47, 3282.
Dirven, H.A., et al. 1995. Chem. Res. Toxicol. 8, 979.
Kolm, R.H., et al. 1995. Biochem. J. 311, 453.
Cameron, A.D., et al. 1995. Structure 3, 717
Talalay, P., et al. 1995. Toxicol. Lett. 82-83, 173.




