Fostriecin is the most fully characterised member of a family of phosphate esters of a triene antibiotic. The antitumor potential of Fostriecin has attracted considerable interest, focused on its mode of action as a topoisomerase II inhibitor. Subsequent research has focused on this metabolite's selective inhibition of protein phosphatase PP2A.
Fostriecin is soluble in water, with optimal stability in aqueous buffered solutions at pH 6.5. NOTE: hydrolysis of the phosphate ester will result from inappropriate storage.
| References | Chromosome condensation induced by fostriecin does not require p34cdc2 kinase activity and histone H1 hyperphosphorylation, but is associated with enhanced histone H2A and H3 phosphorylation. Guo X.W. et al. EMBO J. 1995, 14, 976. Antitumor drug fostriecin inhibits the mitotic entry checkpoint and protein phosphatases 1 and 2A. Roberge M. et al. Cancer Res. 1994, 54, 6115. Fostriecin, an antitumor antibiotic with inhibitory activity against serine/threonine protein phosphatases types 1 (PP1) and 2A (PP2A), is highly selective for PP2A. Walsh A. H. et al. FEBS Lett. 1997, 416, 230. |