Demystifying the potential of inhibitors targeting DNA topoisomerases in unicellular protozoan parasites.

DNA topoisomerases are a group of enzymes omnipresent in all organisms. They maintain the DNA topology during replication, repair, recombination, and transcription. However, the structure of topoisomerase in protozoan parasites differs significantly from that of human topoisomerases; thus, this enzyme acts as a crucial target in drug development against parasitic diseases. Although the therapeutic potential of drugs targeting the parasitic topoisomerase is well known, to manage the shortcomings of currently available therapeutics and the emergence of drug resistance, the discovery of novel antiparasitic molecules is an urgent need. In this review, we describe various investigational and repurposed topoisomerase inhibitors developed against protozoan parasites over the past few years. Copyright © 2023 Elsevier Ltd. All rights reserved.

Citation

Swati Lamba, Amit Roy. Demystifying the potential of inhibitors targeting DNA topoisomerases in unicellular protozoan parasites. Drug discovery today. 2023 Jun;28(6):103574

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PMID: 37003515

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