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Topoisomerase II Catalytic InhibitorsDNA topoisomerase II is a nuclear enzyme which is essential for cell division. The enzyme acts by creating breaks in DNA, thereby allowing the DNA strands to unravel and separate. Topoisomerase II is the molecular target for a number of important anti-cancer drugs which act by preventing the enzyme from resealing the DNA break it creates. This results in an accumulation of double stranded DNA breaks which leads to cell death. Such drugs are known as topoisomerase II poisons.Catalytic inhibitors (CIs) are a second class of compound which target topoisomerase II. However, in contrast to poisons, these drugs act at a point in the enzymes catalytic cycle where DNA breaks do not occur. Importantly, CIs can act as antagonists to poisons, stabilising topoisomerase II in a form which is inaccessible to the poison. Clinically this means that the CI protects the cell from the effects of a Poison. One application of Catalytic Inhibitors has been developed for prevention of severe tissue damage following extravasation of anthracyclines. This application has been discovered, developed and marketed by TopoTarget as Savene® in the European market and Totect® in the US market. Useful links :
- Savene®/Totect®
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Cancer