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Plasmodium falciparum plasmepsin X

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Target id: 3071

Nomenclature: Plasmodium falciparum plasmepsin X

Abbreviated Name: PfPMX

Systematic Nomenclature: Plasmodium falciparum plasmepsin X

Family: Antimalarial targets

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Plasmodium falciparum 3D7 - 573 PMX plasmepsin X
Database Links Click here for help
PlasmoDB
UniProtKB
Other Binding Ligands
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Reference
WM382 Small molecule or natural product Pf Inhibition 10.5 pKi 2
pKi 10.5 (Ki 3.5x10-11 M) [2]
Description: Peptide cleavage assay using recombinant PMX
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
WM382 Small molecule or natural product Pk Parasite growth inhibition assay - - 9.7 pEC50 2
pEC50 9.7 (EC50 1.8x10-10 M) SYBR Green assay [2]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
WM382 Small molecule or natural product PfDd2 Parasite growth inhibition assay - - 9.6 pEC50 2
pEC50 9.6 (EC50 2.6x10-10 M) [2]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
WM382 Small molecule or natural product Pf3D7 Parasite growth inhibition assay - - 9.2 pEC50 2
pEC50 9.2 (EC50 6x10-10 M) Results are for R-WM382 [2]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
WM382 Small molecule or natural product PfK1 Parasite growth inhibition assay - - 9.2 pEC50 2
pEC50 9.2 (EC50 6.5x10-10 M) [2]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
WM382 Small molecule or natural product Pf Standard membrane feeding assay (SMFA) - - - - 2
Oocyst count: potent inhibition of oocyst development [2]
Lifecycle stages: Plasmodium mosquito host stage (gametocyte, gamete, zygote, ookinete, oocyst, sporozoite)
Malaria Pharmacology Comments
The P. falciparum genome encodes 10 aspartic proteases, classed together as the plasmepsin family, which are involved in diverse cellular processes [1]. P. falciparum plasmepsin X (PfPMX) has emerged as a promising target for antimalarial drug development with studies demonstrating an essential role in merozoite invasion and egress of erythrocytes [3-4].

References

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1. Coombs GH, Goldberg DE, Klemba M, Berry C, Kay J, Mottram JC. (2001) Aspartic proteases of Plasmodium falciparum and other parasitic protozoa as drug targets. Trends Parasitol., 17 (11): 532-7. [PMID:11872398]

2. Favuzza P, de Lera Ruiz M, Thompson JK, Triglia T, Ngo A, Steel RWJ, Vavrek M, Christensen J, Healer J, Boyce C et al.. (2020) Dual Plasmepsin-Targeting Antimalarial Agents Disrupt Multiple Stages of the Malaria Parasite Life Cycle. Cell Host Microbe, 27 (4): 642-658.e12. [PMID:32109369]

3. Nasamu AS, Glushakova S, Russo I, Vaupel B, Oksman A, Kim AS, Fremont DH, Tolia N, Beck JR, Meyers MJ et al.. (2017) Plasmepsins IX and X are essential and druggable mediators of malaria parasite egress and invasion. Science, 358 (6362): 518-522. [PMID:29074774]

4. Pino P, Caldelari R, Mukherjee B, Vahokoski J, Klages N, Maco B, Collins CR, Blackman MJ, Kursula I, Heussler V et al.. (2017) A multistage antimalarial targets the plasmepsins IX and X essential for invasion and egress. Science, 358 (6362): 522-528. [PMID:29074775]

How to cite this page

Antimalarial targets: Plasmodium falciparum plasmepsin X. Last modified on 24/08/2020. Accessed on 20/01/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=3071.