|Topo II Inhibitors||Mechanism of Action|
|Liposomal doxorubicin, Doxorubicin, Etoposide, Epirubicin||Inhibits DNA synthesis, RNA transcription, and cell division by blocking activity of topoisomerase II|
- DNA replication and transcription cannot proceed without unwinding of supercoiled DNA mediated by Top2A, which cleaves DNA and covalently attaches to it during this process. Binding of the inhibitor to topo2A-DNA generates a stable ternary complex and results in a double strand DNA break. High levels of Top2A-DNA-drug complexes result in increased DNA damage and cell death.
- PGP pumps doxorubicin and epirubicin out of the cell thereby decreasing its intracellular concentration.
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Green squares, sensitivity markers. Red squares, resistance markers