Question

topoisomerase drugs have been developed (and still developing) to treat different cancers in humans. If you were to develop a drug to target topoisomerase II, which step in its process would be most effective to affect cellular function (assuming it is irreversibly bound)? Why would this be the most effective as a drug?

Answer 1

Topoisomerase is the enzyme which is responsible for relaxing the supercoiling which occurs ahead of replication bubble during the process of DNA replication. The relaxing of supercoiling is important because if it is not relaxed, then the whole DNA ahead of replication bubble will get entangled. There will be difficulty in the formation of more replication Bubbles in the entangled region and therefore the DNA will not be able to replicate itself. Therefore the activity of topoisomerase is important because relaxation of supercoiling is particularly important for DNA replication to proceed normally.

If we develop a drug to target topoisomerase 2, then it will effect the process of DNA replication. Supercoiling will not be relaxed and DNA replication will not proceed normally.

This will be a very effective drug because it is not allowing the cell to undertake DNA replication. In this case the cell will not divide because it does not have DNA which can be distributed equally among the daughter cells. Without cell division, the organism will not be able to carry out its life cycle normally and ultimately will die.

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