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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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Peptidomimetic inhibitors of N-myristoyltransferase from human malaria and leishmaniasis parasites.pdf - Published Version Available under License Creative Commons Attribution. Download (1MB) | Preview |
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 |
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| 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: | 04 Sep 2021 02:37 |
| DOI or ID number: | 10.1039/c4ob01669f |
| URI: | https://researchonline.ljmu.ac.uk/id/eprint/8853 |
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