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Plasmodium falciparum phenylalanine--tRNA ligase alpha subunit

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Target id: 2954

Nomenclature: Plasmodium falciparum phenylalanine--tRNA ligase alpha subunit

Abbreviated Name: PfcPheRS

Family: Aminoacyl-tRNA synthetases

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Plasmodium falciparum 3D7 - 575 cPheRS phenylalanine--tRNA ligase alpha subunit
Previous and Unofficial Names Click here for help
Plasmodium falciparum phenylalanyl-tRNA synthetase alpha subunit | Pfal cPheRS
Database Links Click here for help
PlasmoDB
UniProtKB

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
BRD3444 Small molecule or natural product Pf3D7 Inhibition 7.3 pIC50 1
pIC50 7.3 (IC50 4.6x10-8 M) [1]
Whole Organism Assay Data Linked to This Target
Key to terms and symbols Click column headers to sort
Ligand Sp. Assay description Type Action Value Parameter Reference
BRD3444 Small molecule or natural product PfDd2 Parasite growth inhibition assay - - 8.1 pEC50 1
pEC50 8.1 (EC50 9x10-9 M) SYBR Green I assay [1]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
BRD3444 Small molecule or natural product Pf3D7 Parasite late stage (IV–V) gametocyte assay - - 6.2 pEC50 1
pEC50 6.2 (EC50 6.63x10-7 M) [1]
Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
Malaria Pharmacology Comments
The aminoacyl-tRNA synthetases are emerging targets for antimalarial agents [2]. The target described here (PfcPheRS) is unique in that it is the first member of the class whose inhibition results in elimination of blood (asexual and sexual), liver and transmission stage parasites [1].

References

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1. Kato N, Comer E, Sakata-Kato T, Sharma A, Sharma M, Maetani M, Bastien J, Brancucci NM, Bittker JA, Corey V et al.. (2016) Diversity-oriented synthesis yields novel multistage antimalarial inhibitors. Nature, 538 (7625): 344-349. [PMID:27602946]

2. Manickam Y, Chaturvedi R, Babbar P, Malhotra N, Jain V, Sharma A. (2018) Drug targeting of one or more aminoacyl-tRNA synthetase in the malaria parasite Plasmodium falciparum. Drug Discov Today, 23 (6): 1233-1240. [PMID:29408369]

How to cite this page

Aminoacyl-tRNA synthetases: Plasmodium falciparum phenylalanine--tRNA ligase alpha subunit. Last modified on 15/03/2021. Accessed on 14/05/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2954.