Oxamflatin acts as an inhibitory ligand for the enzyme active site metal ion of mammalian HDAC. HDACs deacetylate histones thereby allowing the histones to wrap DNA more tightly. This interaction affects gene expression. Oxamflatin elevates the expression of the extracellular matrix proteins fibronectin and gelsolin. Oxamflatin upregulates plasminogen activator inhibitor type 2 (PAI-2) expression with concomitant inhibition of urokinase (u-PA) gene and protein expression in HT-1080 and U-937 cells. Additionally, oxamflatin induces apoptosis in P-glyoprotein (Pgp)-positive and Pgp-negative multidrug resistant cells.
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