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

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Olaleye TO, Brannigan JA, Roberts SM, Leatherbarrow RJ, Wilkinson AJ, Tate EW
OpenAccess logo Org Biomol Chem 12 8132-7 (2014)
Related entries: 4c7h, 4c7i

Cited: 20 times
EuropePMC logo PMID: 25230674

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.

Reviews - 4c68 mentioned but not cited (1)

  1. Structure and Functional Diversity of GCN5-Related N-Acetyltransferases (GNAT). Salah Ud-Din AI, Tikhomirova A, Roujeinikova A. Int J Mol Sci 17 E1018 (2016)

Articles - 4c68 mentioned but not cited (2)

  1. Peptidomimetic inhibitors of N-myristoyltransferase from human malaria and leishmaniasis parasites. Olaleye TO, Brannigan JA, Roberts SM, Leatherbarrow RJ, Wilkinson AJ, Tate EW. Org Biomol Chem 12 8132-8137 (2014)
  2. Identification of potent and selective N-myristoyltransferase inhibitors of Plasmodium vivax liver stage hypnozoites and schizonts. Rodríguez-Hernández D, Vijayan K, Zigweid R, Fenwick MK, Sankaran B, Roobsoong W, Sattabongkot J, Glennon EKK, Myler PJ, Sunnerhagen P, Staker BL, Kaushansky A, Grøtli M. Nat Commun 14 5408 (2023)


Reviews citing this publication (4)

  1. Drug target identification in protozoan parasites. Müller J, Hemphill A. Expert Opin Drug Discov 11 815-824 (2016)
  2. New developments in probing and targeting protein acylation in malaria, leishmaniasis and African sleeping sickness. Ritzefeld M, Wright MH, Tate EW. Parasitology 145 157-174 (2018)
  3. Drug discovery in leishmaniasis using protein lipidation as a target. Brannigan JA, Wilkinson AJ. Biophys Rev 13 1139-1146 (2021)
  4. Three-dimensional structures in the design of therapeutics targeting parasitic protozoa: reflections on the past, present and future. Hol WG. Acta Crystallogr F Struct Biol Commun 71 485-499 (2015)

Articles citing this publication (13)

  1. Global analysis of protein N-myristoylation and exploration of N-myristoyltransferase as a drug target in the neglected human pathogen Leishmania donovani. Wright MH, Paape D, Storck EM, Serwa RA, Smith DF, Tate EW. Chem Biol 22 342-354 (2015)
  2. High-resolution snapshots of human N-myristoyltransferase in action illuminate a mechanism promoting N-terminal Lys and Gly myristoylation. Dian C, Pérez-Dorado I, Rivière F, Asensio T, Legrand P, Ritzefeld M, Shen M, Cota E, Meinnel T, Tate EW, Giglione C. Nat Commun 11 1132 (2020)
  3. Global Profiling and Inhibition of Protein Lipidation in Vector and Host Stages of the Sleeping Sickness Parasite Trypanosoma brucei. Wright MH, Paape D, Price HP, Smith DF, Tate EW. ACS Infect Dis 2 427-441 (2016)
  4. N-myristoyltransferase is a cell wall target in Aspergillus fumigatus. Fang W, Robinson DA, Raimi OG, Blair DE, Harrison JR, Lockhart DE, Torrie LS, Ruda GF, Wyatt PG, Gilbert IH, van Aalten DM. ACS Chem Biol 10 1425-1434 (2015)
  5. Discovery of high affinity inhibitors of Leishmania donovani N-myristoyltransferase. Rackham MD, Yu Z, Brannigan JA, Heal WP, Paape D, Barker KV, Wilkinson AJ, Smith DF, Leatherbarrow RJ, Tate EW. Medchemcomm 6 1761-1766 (2015)
  6. Structure-Guided Identification of Resistance Breaking Antimalarial N‑Myristoyltransferase Inhibitors. Schlott AC, Mayclin S, Reers AR, Coburn-Flynn O, Bell AS, Green J, Knuepfer E, Charter D, Bonnert R, Campo B, Burrows J, Lyons-Abbott S, Staker BL, Chung CW, Myler PJ, Fidock DA, Tate EW, Holder AA. Cell Chem Biol 26 991-1000.e7 (2019)
  7. Novel Thienopyrimidine Inhibitors of Leishmania N-Myristoyltransferase with On-Target Activity in Intracellular Amastigotes. Bell AS, Yu Z, Hutton JA, Wright MH, Brannigan JA, Paape D, Roberts SM, Sutherell CL, Ritzefeld M, Wilkinson AJ, Smith DF, Leatherbarrow RJ, Tate EW. J Med Chem 63 7740-7765 (2020)
  8. Structure-guided optimization of quinoline inhibitors of Plasmodium N-myristoyltransferase. Goncalves V, Brannigan JA, Laporte A, Bell AS, Roberts SM, Wilkinson AJ, Leatherbarrow RJ, Tate EW. Medchemcomm 8 191-197 (2017)
  9. Exploring Novel N-Myristoyltransferase Inhibitors: A Molecular Dynamics Simulation Approach. Khalil R, Ashraf S, Khalid A, Ul-Haq Z. ACS Omega 4 13658-13670 (2019)
  10. Discovery of pyridyl-based inhibitors of Plasmodium falciparum N-myristoyltransferase. Yu Z, Brannigan JA, Rangachari K, Heal WP, Wilkinson AJ, Holder AA, Leatherbarrow RJ, Tate EW. Medchemcomm 6 1767-1772 (2015)
  11. Identification of Potential Leishmania N-Myristoyltransferase Inhibitors from Withania somnifera (L.) Dunal: A Molecular Docking and Molecular Dynamics Investigation. Orabi MAA, Alshahrani MM, Sayed AM, Abouelela ME, Abouelela ME, Shaaban KA, Abdel-Sattar ES. Metabolites 13 93 (2023)
  12. Identification of and Structural Insights into Hit Compounds Targeting N-Myristoyltransferase for Cryptosporidium Drug Development. Fenwick MK, Reers AR, Liu Y, Zigweid R, Sankaran B, Shin J, Hulverson MA, Hammerson B, Fernández Álvaro E, Myler PJ, Kaushansky A, Van Voorhis WC, Fan E, Staker BL. ACS Infect Dis 9 1821-1833 (2023)
  13. Screening of medicinal plants unraveled the leishmanicidal credibility of Garcinia cowa; highlighting Norcowanin, a novel anti-leishmanial phytochemical through in-silico study. Pyne N, Paul S. J Parasit Dis 46 202-214 (2022)


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