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Plasmodium falciparum plasmepsin V

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Target id: 3106

Nomenclature: Plasmodium falciparum plasmepsin V

Abbreviated Name: PfPMV

Family: Plasmepsin family (peptidases)

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Plasmodium falciparum 3D7 - 590 PMV plasmepsin V
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ChEMBL Target
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
WEHI-842 Small molecule or natural product Ligand has a PDB structure PfNF54 Parasite gametocyte assay - - 7.4 pEC50 4
pEC50 7.4 (EC50 4x10-8 M) Giemsa-stained blood film counts: no stage II-V gametocytes were observed [4]
WEHI-842 Small molecule or natural product Ligand has a PDB structure Pf3D7 - - 6.4 pEC50 3
pEC50 6.4 (EC50 4x10-7 M) [3]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Malaria Pharmacology Comments
The P. falciparum plasmepsin V (PfPMV) enzyme processes proteins for export into the host erythrocyte and has been shown to be essential for parasite asexual blood stage development [1-2]. PfPMV has also been shown to be essential for gametocyte development, validating it as a potential target for the development of transmission-blocking drugs [4].

References

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1. Boddey JA, Hodder AN, Günther S, Gilson PR, Patsiouras H, Kapp EA, Pearce JA, de Koning-Ward TF, Simpson RJ, Crabb BS et al.. (2010) An aspartyl protease directs malaria effector proteins to the host cell. Nature, 463 (7281): 627-31. [PMID:20130643]

2. Boonyalai N, Collins CR, Hackett F, Withers-Martinez C, Blackman MJ. (2018) Essentiality of Plasmodium falciparum plasmepsin V. PLoS ONE, 13 (12): e0207621. [PMID:30517136]

3. Hodder AN, Sleebs BE, Czabotar PE, Gazdik M, Xu Y, O'Neill MT, Lopaticki S, Nebl T, Triglia T, Smith BJ et al.. (2015) Structural basis for plasmepsin V inhibition that blocks export of malaria proteins to human erythrocytes. Nat Struct Mol Biol, 22 (8): 590-6. [PMID:26214367]

4. Jennison C, Lucantoni L, O'Neill MT, McConville R, Erickson SM, Cowman AF, Sleebs BE, Avery VM, Boddey JA. (2019) Inhibition of Plasmepsin V Activity Blocks Plasmodium falciparum Gametocytogenesis and Transmission to Mosquitoes. Cell Rep, 29 (12): 3796-3806.e4. [PMID:31851913]

How to cite this page

Plasmepsin family (peptidases): Plasmodium falciparum plasmepsin V. Last modified on 15/02/2021. Accessed on 12/05/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=3106.