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2006 | 53 | 3 | 547-552
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Tocopherol esters inhibit human glutathione S-transferase omega

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Human glutathione S-transferase omega 1-1 (hGSTO1-1) is a newly identified member of the glutathione S-transferase (GST) family of genes, which also contains alpha, mu, pi, sigma, theta, and zeta members. hGSTO1-1 catalyzes the reduction of arsenate, monomethylarsenate (MMA(V)), and dimethylarsenate (DMA(V)) and exhibits thioltransferase and dehydroascorbate reductase activities. Recent evidence has show that cytokine release inhibitory drugs, which specifically inhibit interleukin-1b (IL-1b), directly target hGSTO1-1. We found that (+)-α-tocopherol phosphate and (+)-α-tocopherol succinate inhibit hGSTO1-1 in a concentration-dependent manner with IC50 values of 2 µM and 4 µM, respectively. A Lineweaver-Burk plot demonstrated the uncompetitive nature of this inhibition. The molecular mechanism behind the inhibition of hGSTO1-1 by α-tocopherol esters (vitamin E) is important for understanding neurodegenerative diseases, which are also influenced by vitamin E.
Physical description
  • División de Farmacología y Toxicología, Centro de Investigación Biomédica del Noreste, Instituto Mexicano del Seguro Social, Monterrey, Nuevo León, México
  • Department of Molecular and Cellular Biology; The University of Arizona, Tucson, Arizona, USA
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