Plasmodium falciparum N-Myristoyltransferase | Antimalarial targets | IUPHAR/BPS Guide to PHARMACOLOGY

Plasmodium falciparum N-Myristoyltransferase

Target id: 2955

Nomenclature: Plasmodium falciparum N-Myristoyltransferase

Abbreviated Name: PfNMT

Family: Antimalarial targets

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for Plasmodium falciparum N-Myristoyltransferase in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Plasmodium falciparum 3D7 - 410 NMT glycylpeptide N-tetradecanoyltransferaselength
Previous and Unofficial Names
Pfal NMT
Database Links
UniProtKB

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
Ligand Sp. Action Affinity Units Reference
Compound 34c [PMID 24641010] Pf3D7 Inhibition 8.1 pKi 1
pKi 8.1 (Ki 8x10-9 M) [1]
Description: Enzyme inhibition assay
Whole Organism Assay Data Linked to This Target
Key to terms and symbols Click column headers to sort
Ligand Sp. Assay description Type Action Affinity Units Reference
Compound 34c [PMID 24641010] PfNF54 Parasite growth inhibition assay - - 6.6 pEC50 1
pEC50 6.6 (EC50 2.32x10-7 M) [3H]-hypoxanthine incorporation [1]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Compound 34c [PMID 24641010] Pf3D7 Parasite growth inhibition assay - - 6.5 pEC50 1
pEC50 6.5 (EC50 3.02x10-7 M) [3H]-hypoxanthine incorporation [1]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Compound 34c [PMID 24641010] PfK1 Parasite growth inhibition assay - - 6.5 pEC50 1
pEC50 6.5 (EC50 3.39x10-7 M) [3H]-hypoxanthine incorporation [1]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Compound 34c [PMID 24641010] Pb Parasite liver stage assay - - 6.4 pEC50 1
pEC50 6.4 (EC50 3.72x10-7 M) Luciferase bioluminescence assay to measure viability of exoerythrocytic forms (EEF) [1]
Lifecycle stages: Plasmodium liver stage (sporozoite, hepatic schizont, hepatic merozoite)
Compound 34c [PMID 24641010] PfDd2 Parasite growth inhibition assay - - 6.0 pEC50 1
pEC50 6.0 (EC50 9.16x10-7 M) [3H]-hypoxanthine incorporation [1]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
General Comments
Genetic essentiality and validation of N-Myristoyltransferase (NMT) as a chemically tractable antimalarial drug target in Plasmodium has been reported. Small molecule on-target inhibition of myristoylation disrupts the function of multiple specific downstream pathways, resulting in rapid cell death [1-2].

References

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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. 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]

How to cite this page

Antimalarial targets: Plasmodium falciparum N-Myristoyltransferase. Last modified on 18/07/2018. Accessed on 15/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2955.