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Plasmodium falciparum elongation factor 2

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Target id: 2975

Nomenclature: Plasmodium falciparum elongation factor 2

Abbreviated Name: PfeEF2

Family: Ribosomal factors (Plasmodium spp.)

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Plasmodium falciparum 3D7 - 832 eEF2 elongation factor 2
Gene and Protein Information Comments
Our eukaryotic translation elongation factor 2 summary page provides information about the homologous human target.
Previous and Unofficial Names Click here for help
PF14_0486
Database Links Click here for help
Alphafold
PlasmoDB
UniProtKB
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
M5717 Small molecule or natural product Guide to Malaria Pharmacology Ligand Pf3D7 Parasite growth inhibition assay - - 9.0 pEC50 1
pEC50 9.0 (EC50 1x10-9 M) [3H]-hypoxanthine incorporation assay [1]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
M5717 Small molecule or natural product Guide to Malaria Pharmacology Ligand PfNF54 Parasite gamete formation assay - - 8.7 – 8.9 pEC50 1
pEC50 8.9 (EC50 1.2x10-9 M) Female gamete formation [1]
Lifecycle stages: Plasmodium mosquito host stage (gametocyte, gamete, zygote, ookinete, oocyst, sporozoite)
pEC50 8.7 (EC50 1.8x10-9 M) Male gamete formation [1]
Lifecycle stages: Plasmodium mosquito host stage (gametocyte, gamete, zygote, ookinete, oocyst, sporozoite)
M5717 Small molecule or natural product Guide to Malaria Pharmacology Ligand Pb Parasite liver stage assay - - 8.8 pEC50 1
pEC50 8.8 (EC50 1.65x10-9 M) P. berghei Luciferase liver stage assay [1]
Lifecycle stages: Plasmodium liver stage (sporozoite, hepatic schizont, hepatic merozoite)
M5717 Small molecule or natural product Guide to Malaria Pharmacology Ligand PfNF54 Standard membrane feeding assay (SMFA) - - 8.0 – 8.7 pEC50 1
pEC50 8.7 (EC50 1.8x10-9 M) Indirect SMFA [1]
Lifecycle stages: Plasmodium mosquito host stage (gametocyte, gamete, zygote, ookinete, oocyst, sporozoite)
pEC50 8.0 (EC50 1x10-8 M) Direct SMFA [1]
Lifecycle stages: Plasmodium mosquito host stage (gametocyte, gamete, zygote, ookinete, oocyst, sporozoite)
Malaria Pharmacology Comments
Elongation factor 2 (eEF2) catalyzes the GTP-dependent translocation of the ribosome along messenger RNA, and is essential for protein synthesis in eukaryotes. Studies in S. cerevisiae have shown that this highly conserved protein is the target for the antifungal compound sordarin [3-4], while Plasmodium eEF2 (PfeEF2) has been identified as a novel target for antimalarial drug development [1] and a key target for interruption of malaria transmission [2].

References

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1. Baragaña B, Hallyburton I, Lee MC, Norcross NR, Grimaldi R, Otto TD, Proto WR, Blagborough AM, Meister S, Wirjanata G et al.. (2015) A novel multiple-stage antimalarial agent that inhibits protein synthesis. Nature, 522 (7556): 315-20. [PMID:26085270]

2. Dechering KJ, Duerr HP, Koolen KMJ, Gemert GV, Bousema T, Burrows J, Leroy D, Sauerwein RW. (2017) Modelling mosquito infection at natural parasite densities identifies drugs targeting EF2, PI4K or ATP4 as key candidates for interrupting malaria transmission. Sci Rep, 7 (1): 17680. [PMID:29247222]

3. Justice MC, Hsu MJ, Tse B, Ku T, Balkovec J, Schmatz D, Nielsen J. (1998) Elongation factor 2 as a novel target for selective inhibition of fungal protein synthesis. J Biol Chem, 273 (6): 3148-51. [PMID:9452424]

4. Shastry M, Nielsen J, Ku T, Hsu MJ, Liberator P, Anderson J, Schmatz D, Justice MC. (2001) Species-specific inhibition of fungal protein synthesis by sordarin: identification of a sordarin-specificity region in eukaryotic elongation factor 2. Microbiology (Reading), 147 (Pt 2): 383-390. [PMID:11158355]

How to cite this page

Ribosomal factors (Plasmodium spp.): Plasmodium falciparum elongation factor 2. Last modified on 13/10/2021. Accessed on 17/08/2022. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2975.