4.8 Article

Identification of Potent and Selective Non-covalent Inhibitors of the Plasmodium falciparum Proteasome

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JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
卷 136, 期 39, 页码 13562-13565

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AMER CHEMICAL SOC
DOI: 10.1021/ja507692y

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  1. National Institutes of Health [R01 AI078947, R21 AI088541]
  2. National Science Scholarship from the Agency of Science, Technology and Research, Singapore

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We have identified short N,C-capped peptides that selectively inhibit the proteasome of the malaria-causing pathogen Plasmodium falciparum. These compounds are highly potent in culture with no toxicity in host cells. One cyclic biphenyl ether compound inhibited intraerythrocytic growth of P. falciparum with an IC50 of 35 nM, and we show that even a pulse treatment with this cyclic peptide induced parasite death due to proteasome inhibition. These compounds represent promising new antimalarial agents that target the essential proteasomal machinery of the parasite without toxicity toward the host

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