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

Olaleye, TO, Brannigan, JA, Roberts, SM, Leatherbarrow, RJ, Wilkinson, AJ and Tate, EW (2014) Peptidomimetic inhibitors of N-myristoyltransferase from human malaria and leishmaniasis parasites. Organic & Biomolecular Chemistry, 12 (41). pp. 8132-8137. ISSN 1477-0520

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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.

Item Type: Article
Uncontrolled Keywords: 0304 Medicinal And Biomolecular Chemistry, 0305 Organic Chemistry, 1115 Pharmacology And Pharmaceutical Sciences
Subjects: Q Science > QD Chemistry
Q Science > QR Microbiology
R Medicine > RM Therapeutics. Pharmacology
Divisions: Vice-Chancellor's Office
Publisher: Royal Society of Chemistry
Related URLs:
Date Deposited: 19 Jun 2018 11:01
Last Modified: 15 Sep 2018 18:48
DOI or Identification number: 10.1039/c4ob01669f
URI: http://researchonline.ljmu.ac.uk/id/eprint/8853

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