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ID: ALA1133240

Journal: Bioorg Med Chem Lett

Title: Michael adducts of ascorbic acid as inhibitors of protein phosphatase 2A and inducers of apoptosis.

Authors: Fathi AR, Krautheim A, Kaap S, Eger K, Steinfelder HJ.

Abstract: Michael adducts of ascorbic acid with alpha,beta-unsaturated carbonyl compounds have been shown to be potent inhibitors of protein phosphatase 1 (PP1) without affecting cell viability at the respective concentrations. Here we were able to show that higher concentrations can partially inhibit PP2A activity and concomitantly induce apoptotic cell death. A nitrostyrene adduct of ascorbic acid proved to be a more potent and effective inhibitor of PP2A as well as a stronger inducer of apoptosis. These adducts only slightly lost their cytotoxic potential in multidrug resistant cells that were 10-fold less sensitive to apoptosis induction by okadaic acid and vinblastine.

CiteXplore: 10915062

DOI: 10.1016/s0960-894x(00)00294-8