Plasmodium falciparum N-Myristoyltransferase

Target id: 2955

Nomenclature: Plasmodium falciparum N-Myristoyltransferase

Abbreviated Name: Pfal NMT

Family: Anti-infective 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 - 410 NMT glycylpeptide N-tetradecanoyltransferaselength
Database Links
UniProtKB

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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] Pfal Inhibition 8.1 pKi 1
pKi 8.1 (Ki 8x10-9 M) The parasite EC50 against Pfal was 305 nM [1]
General Comments
Genetic essentiality and validation of NMT as a chemically tractable 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].

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]

How to cite this page

Anti-infective targets: Plasmodium falciparum N-Myristoyltransferase. Last modified on 21/08/2017. Accessed on 18/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2955.