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Prospects of Topoisomerase Inhibitors as Promising Anti-Cancer Agents

Topoisomerases are very important enzymes that regulate DNA topology and are vital for biological actions like DNA replication, transcription, and repair. The emergence and spread of cancer has been intimately associated with topoisomerase dysregulation. Topoisomerase inhibitors have consequently become potential anti-cancer medications because of their ability to obstruct the normal function of these enzymes, which leads to DNA damage and subsequently causes cell death. This review emphasizes the importance of topoisomerase inhibitors as marketed, clinical and preclinical anti-cancer medications. In the present review, various types of topoisomerase inhibitors and their mechanisms of action have been discussed. Topoisomerase I inhibitors, which include irinotecan and topotecan, are agents that interact with the DNA-topoisomerase I complex and avert resealing of the DNA. The accretion of DNA breaks leads to the inhibition of DNA replication and cell death. On the other hand, topoisomerase II inhibitors like etoposide and teniposide, function by cleaving the DNA-topoisomerase II complex thereby effectively impeding the release of double-strand DNA breaks. Moreover, the recent advances in exploring the therapeutic efficacy, toxicity, and MDR (multidrug resistance) issues of new topoisomerase inhibitors have been reviewed in the present review.

 

Comments:

Your summary provides a comprehensive overview of the importance of topoisomerases and their inhibitors in cancer treatment. Topoisomerases play a crucial role in DNA replication, transcription, and repair, and their dysregulation has been linked to the emergence and spread of cancer. Inhibitors of these enzymes have become potential anti-cancer medications due to their ability to disrupt normal enzymatic function, leading to DNA damage and cell death.

The review discusses different types of topoisomerase inhibitors and their mechanisms of action. Topoisomerase I inhibitors, such as irinotecan and topotecan, prevent the resealing of DNA breaks, leading to the accumulation of breaks, inhibition of DNA replication, and ultimately, cell death. On the other hand, topoisomerase II inhibitors like etoposide and teniposide work by cleaving the DNA-topoisomerase II complex, hindering the release of double-strand DNA breaks.

Additionally, the review covers recent advances in understanding the therapeutic efficacy, toxicity, and multidrug resistance issues associated with new topoisomerase inhibitors. This information highlights the ongoing research efforts to develop effective and safe anti-cancer medications targeting topoisomerases.

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S1787 Teniposide Teniposide (NSC 122819, VM-26) is a chemotherapeutic medication mainly used in the treatment of childhood acute lymphocytic leukemia (ALL).

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Topoisomerase