Topoisomerase II from Human Malaria Parasites

  • Mudeppa D
  • Kumar S
  • Kokkonda S
  • et al.
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Abstract

Background: Topoisomerase II-disabling antibacterials and anticancer drugs exist but not antimalarials. Results: Engineered Plasmodium falciparum topoisomerase II (PfTopoII) led to a functional enzyme and to early inhibitors with antimalarial properties in cell-based assays. Conclusion: Pure, stable PfTopoII is now ready for advanced HTS and lead optimization studies. Significance: This biochemical platform should help accelerate antimalarial drug discovery.

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Mudeppa, D. G., Kumar, S., Kokkonda, S., White, J., & Rathod, P. K. (2015). Topoisomerase II from Human Malaria Parasites. Journal of Biological Chemistry, 290(33), 20313–20324. https://doi.org/10.1074/jbc.m115.639039

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