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Target id: 2955
Nomenclature: Plasmodium falciparum N-myristoyltransferase
Abbreviated Name: PfNMT
Family: Other antimalarial targets
Gene and Protein Information | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Plasmodium falciparum 3D7 | - | 410 | NMT | glycylpeptide N-tetradecanoyltransferase | ||
Gene and Protein Information Comments | ||||||
The P. falciparum genome encodes a single NMT isoform that is 50% identical to, and shares key catalytic residues with, human NMT. |
Database Links | |
Alphafold | Q8ILW6 (Pf3D7) |
ChEMBL Target | CHEMBL2169722 (Pf3D7) |
PlasmoDB | PF3D7_1412800 (Pf3D7) |
UniProtKB | Q8ILW6 (Pf3D7) |
Download all structure-activity data for this target as a CSV file
Inhibitors | |||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||
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Whole Organism Assay Data Linked to This Target | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Malaria Pharmacology Comments |
The enzyme N-myristoyltransferase (NMT) catalyses cotranslational transfer of myristic acid from myristoyl coenzyme A to an N-terminal glycine. Genetic essentiality and validation of P. falciparum N-myristoyltransferase (PfNMT) as a chemically tractable antimalarial drug target has been reported. Small molecule on-target inhibition of myristoylation disrupts the function of multiple specific downstream pathways, resulting in rapid cell death [1,3]. |
1. Rackham MD, Brannigan JA, Rangachari K, Meister S, Wilkinson AJ, Holder AA, Leatherbarrow RJ, Tate EW. (2014) Design and synthesis of high affinity inhibitors of Plasmodium falciparum and Plasmodium vivax N-myristoyltransferases directed by ligand efficiency dependent lipophilicity (LELP). J Med Chem, 57 (6): 2773-88. [PMID:24641010]
2. Schlott AC, Mayclin S, Reers AR, Coburn-Flynn O, Bell AS, Green J, Knuepfer E, Charter D, Bonnert R, Campo B et al.. (2019) Structure-Guided Identification of Resistance Breaking Antimalarial N‑Myristoyltransferase Inhibitors. Cell Chem Biol, 26 (7): 991-1000.e7. [PMID:31080074]
3. Wright MH, Clough B, Rackham MD, Rangachari K, Brannigan JA, Grainger M, Moss DK, Bottrill AR, Heal WP, Broncel M et al.. (2014) Validation of N-myristoyltransferase as an antimalarial drug target using an integrated chemical biology approach. Nat Chem, 6 (2): 112-21. [PMID:24451586]
Other antimalarial targets: Plasmodium falciparum N-myristoyltransferase. Last modified on 29/03/2022. Accessed on 11/11/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2955.