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Design and synthesis of inhibitors of Plasmodium falciparum N-myristoyltransferase, a promising target for antimalarial drug discovery.

Yu Z, Brannigan JA, Moss DK, Brzozowski AM, Wilkinson AJ, Holder AA, Tate EW, Leatherbarrow RJ
J Med Chem 55 8879-90 (2012)
Related entries: 4b10, 4b12, 4b13, 4b14

Cited: 38 times
EuropePMC logo PMID: 23035716

Abstract

Design of inhibitors for N-myristoyltransferase (NMT), an enzyme responsible for protein trafficking in Plasmodium falciparum , the most lethal species of parasites that cause malaria, is described. Chemistry-driven optimization of compound 1 from a focused NMT inhibitor library led to the identification of two early lead compounds 4 and 25, which showed good enzyme and cellular potency and excellent selectivity over human NMT. These molecules provide a valuable starting point for further development.

Reviews - 4b11 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 - 4b11 mentioned but not cited (8)

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  4. Design and synthesis of inhibitors of Plasmodium falciparum N-myristoyltransferase, a promising target for antimalarial drug discovery. Yu Z, Brannigan JA, Moss DK, Brzozowski AM, Wilkinson AJ, Holder AA, Tate EW, Leatherbarrow RJ. J Med Chem 55 8879-8890 (2012)
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Reviews citing this publication (6)

  1. N-Myristoyltransferase as a potential drug target in malaria and leishmaniasis. Tate EW, Bell AS, Rackham MD, Wright MH. Parasitology 141 37-49 (2014)
  2. Repurposing strategies for tropical disease drug discovery. Klug DM, Gelb MH, Pollastri MP. Bioorg Med Chem Lett 26 2569-2576 (2016)
  3. Drug target identification in protozoan parasites. Müller J, Hemphill A. Expert Opin Drug Discov 11 815-824 (2016)
  4. 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)
  5. Chemical proteomics: a powerful tool for exploring protein lipidation. Storck EM, Serwa RA, Tate EW. Biochem Soc Trans 41 56-61 (2013)
  6. From crystal to compound: structure-based antimalarial drug discovery. Drinkwater N, McGowan S. Biochem J 461 349-369 (2014)

Articles citing this publication (23)

  1. Structure-based design of potent and selective Leishmania N-myristoyltransferase inhibitors. Hutton JA, Goncalves V, Brannigan JA, Paape D, Wright MH, Waugh TM, Roberts SM, Bell AS, Wilkinson AJ, Smith DF, Leatherbarrow RJ, Tate EW. J Med Chem 57 8664-8670 (2014)
  2. N-Myristoyltransferase Inhibition Induces ER-Stress, Cell Cycle Arrest, and Apoptosis in Cancer Cells. Thinon E, Morales-Sanfrutos J, Mann DJ, Tate EW. ACS Chem Biol 11 2165-2176 (2016)
  3. Design and synthesis of high affinity inhibitors of Plasmodium falciparum and Plasmodium vivax N-myristoyltransferases directed by ligand efficiency dependent lipophilicity (LELP). Rackham MD, Brannigan JA, Rangachari K, Meister S, Wilkinson AJ, Holder AA, Leatherbarrow RJ, Tate EW. J Med Chem 57 2773-2788 (2014)
  4. Unique apicomplexan IMC sub-compartment proteins are early markers for apical polarity in the malaria parasite. Poulin B, Patzewitz EM, Brady D, Silvie O, Wright MH, Ferguson DJ, Wall RJ, Whipple S, Guttery DS, Tate EW, Wickstead B, Holder AA, Tewari R. Biol Open 2 1160-1170 (2013)
  5. Discovery of novel and ligand-efficient inhibitors of Plasmodium falciparum and Plasmodium vivax N-myristoyltransferase. Rackham MD, Brannigan JA, Moss DK, Yu Z, Wilkinson AJ, Holder AA, Tate EW, Leatherbarrow RJ. J Med Chem 56 371-375 (2013)
  6. Synthesis of polysubstituted benzofuran derivatives as novel inhibitors of parasitic growth. Thévenin M, Thoret S, Grellier P, Dubois J. Bioorg Med Chem 21 4885-4892 (2013)
  7. 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)
  8. 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)
  9. 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)
  10. Recent advances in the discovery of N-myristoyltransferase inhibitors. Zhao C, Ma S. ChemMedChem 9 2425-2437 (2014)
  11. 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)
  12. Design and Synthesis of Brain Penetrant Trypanocidal N-Myristoyltransferase Inhibitors. Bayliss T, Robinson DA, Smith VC, Brand S, McElroy SP, Torrie LS, Mpamhanga C, Norval S, Stojanovski L, Brenk R, Frearson JA, Read KD, Gilbert IH, Wyatt PG. J Med Chem 60 9790-9806 (2017)
  13. 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)
  14. 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)
  15. An improved method and cost effective strategy for soluble expression and purification of human N-myristoyltransferase 1 in E. coli. Kumar S, Sharma RK. Mol Cell Biochem 392 175-186 (2014)
  16. Inhibition of protein N-myristoylation blocks Plasmodium falciparum intraerythrocytic development, egress and invasion. Schlott AC, Knuepfer E, Green JL, Hobson P, Borg AJ, Morales-Sanfrutos J, Perrin AJ, Maclachlan C, Collinson LM, Snijders AP, Tate EW, Holder AA. PLoS Biol 19 e3001408 (2021)
  17. Integrated machine learning, molecular docking and 3D-QSAR based approach for identification of potential inhibitors of trypanosomal N-myristoyltransferase. Singh N, Shah P, Dwivedi H, Mishra S, Tripathi R, Sahasrabuddhe AA, Siddiqi MI. Mol Biosyst 12 3711-3723 (2016)
  18. Stacking with No Planarity? Gunaydin H, Bartberger MD. ACS Med Chem Lett 7 341-344 (2016)
  19. 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)
  20. Intramolecular oxidative coupling: I2/TBHP/NaN3-mediated synthesis of benzofuran derivatives. Xu W, Li Q, Cao C, Zhang F, Zheng H. Org Biomol Chem 13 6158-6161 (2015)
  21. 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)
  22. Inhibitor Trapping in N-Myristoyltransferases as a Mechanism for Drug Potency. Spassov DS, Atanasova M, Doytchinova I. Int J Mol Sci 24 11610 (2023)
  23. Structure of N-myristoyltransferase from Aspergillus fumigatus. Shimada T, Suzuki M, Katakura S. Acta Crystallogr D Biol Crystallogr 71 754-761 (2015)


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