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Peptidomimetic inhibitors of N-myristoyltransferase from human malaria and leishmaniasis parasites

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JournalOrganic and Biomolecular Chemistry
DateE-pub ahead of print - 10 Sep 2014
DatePublished (current) - 7 Nov 2014
Issue number41
Volume12
Number of pages6
Pages (from-to)8132-8137
Early online date10/09/14
Original languageEnglish

Abstract

N-Myristoyltransferase (NMT) has been shown to be essential in Leishmania and subsequently validated as a drug target in Plasmodium. Herein, we discuss the use of antifungal NMT inhibitors as a basis for inhibitor development resulting in the first sub-micromolar peptidomimetic inhibitors of Plasmodium and Leishmania NMTs. High-resolution structures of these inhibitors with Plasmodium and Leishmania NMTs permit a comparative analysis of binding modes, and provide the first crystal structure evidence for a ternary NMT-Coenzyme A/myristoylated peptide product complex. This journal is

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