Peptide Inhibition of Topoisomerase IB from Plasmodium falciparum

摘要: Control of diseases inflicted by protozoan parasites such as Leishmania, Trypanosoma, and Plasmodium, which pose a serious threat to human health worldwide, depends on rather small number antiparasite drugs, many are toxic and/or inefficient. Moreover, the increasing occurrence drug-resistant emphasizes need for new effective antiprotozoan drugs. In current study, we describe synthetic peptide, WRWYCRCK, with inhibitory effect essential enzyme topoisomerase I from malaria-causing parasite Plasmodium falciparum. The peptide inhibits specifically transition noncovalent covalent DNA binding P. falciparum I, while it does not affect ligation step catalysis. A mechanistic explanation this inhibition is provided molecular docking analyses. Taken together presented results suggest that peptides may represent class potential