Thiosemicarbazones (TSCs) has been shown as noncompetitive inhibitors of human Topoisomerase IIα (TopoIIα). Metal-TSC complexes demonstrated higher activities than their ligands. Metal-TSC was shown to bind on TopoIIα near the ATP binding pocket. Thus in the absence of ATP, metal-TSC complexes can increase TopoIIα-induced cleavage complexes, unlike other inhibitors of TopoIIα. The metal ions of TSC play a predominant role in the activity of TSCs. Cu-TSC complexes are the most active ones compared to their Pd and Pt counterpart. In this study, we study the activity of metal-TSC effects on TopoIIα in the presence and absence of ATP molecule and try to understand the mechanism how metal-TSC interact with TopoIIα.

Mechanism studies of thiosemicarbazone inhibition on human topoisomerase IIα

2019 Spring National Meeting

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