Peptide Inhibition of Topoisomerase IB from Plasmodium falciparum

Autor: Rune R. Laursen, Amit Roy, Ilda D'Annessa, Birgitta R. Knudsen, Alessandro Desideri, Christine J. F. Nielsen, Felicie F. Andersen, David Tordrup
Jazyk: angličtina
Rok vydání: 2011
Předmět:
Zdroj: Molecular Biology International
Roy, A, D'Annessa, I, Nielsen, C J F, Tordrup, D P, Laursen, R R, Andersen, F F, Desideri, A & Knudsen, B R 2011, ' Peptide Inhibition of Topoisomerase IB from Plasmodium falciparum. ', Molecular Biology International, pp. 854626 . https://doi.org/10.4061/2011/854626
ISSN: 2090-2190
2090-2182
Popis: Control of diseases inflicted by protozoan parasites such asLeishmania, Trypanosoma, andPlasmodium, which pose a serious threat to human health worldwide, depends on a rather small number of antiparasite drugs, of which many are toxic and/or inefficient. Moreover, the increasing occurrence of drug-resistant parasites emphasizes the need for new and effective antiprotozoan drugs. In the current study, we describe a synthetic peptide, WRWYCRCK, with inhibitory effect on the essential enzyme topoisomerase I from the malaria-causing parasitePlasmodium falciparum.The peptide inhibits specifically the transition from noncovalent to covalent DNA binding ofP. falciparumtopoisomerase I, while it does not affect the ligation step of catalysis. A mechanistic explanation for this inhibition is provided by molecular docking analyses. Taken together the presented results suggest that synthetic peptides may represent a new class of potential antiprotozoan drugs.
Databáze: OpenAIRE
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