Gene and Protein Information
Species	TM	AA	Chromosomal Location	Gene Symbol	Gene Name	Reference
Plasmodium falciparum 3D7	-	573		PMX	plasmepsin X

Database Links
PlasmoDB	PF3D7_0808200 (Pf3D7)
UniProtKB	Q8IAS0

Other Binding Ligands
Key to terms and symbols		Click column headers to sort
Ligand Sp. Action Value Parameter Reference WM382 Pf Plasmodium falciparum P. falciparum (Pf) is one of five protozoan parasite species of the genus Plasmodium that cause malaria in humans. Pf is responsible for the majority of malaria related deaths and is the most prevalent species in sub-Saharan Africa. ✖ 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 Pk Plasmodium knowlesi P. knowlesi (Pk) is one of five protozoan parasite species of the genus Plasmodium that cause malaria in humans. This species of the parasite was originally identified as causing simian malaria but it is becoming a significant cause of zoonotic malaria and is an emerging public health issue in Southeast Asia. Pk has a 24-hour asexual replication cycle in erythrocytes and can progress quickly to severe clinical disease with fatal cases reported. ✖ 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 PfDd2 Plasmodium falciparum Dd2 P. falciparum strain Dd2 (PfDd2) is a clone derived from PfW2, following continuous culture in mefloquine. PfW2 was cloned from the Indochina III/CDC isolate, originally derived from a Laotian patient who failed chloroquine therapy. PfDd2 can be obtained from the Malaria Research and Reference Reagent Resource Center (MR4) and is reported to be resistant to chloroquine, pyrimethamine and mefloquine. ✖ 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 Pf3D7 Plasmodium falciparum 3D7 P. falciparum strain 3D7 (Pf3D7) was derived from isolate NF54 by limiting dilution. The complete genome of Pf3D7 has been sequenced (GenBank: LN999946.1). Pf3D7 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4) and is sensitive to a panel of antimalarial compounds including chloroquine and pyrimethamine. ✖ 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 PfK1 Plasmodium falciparum K1 P. falciparum strain K1 (PfK1) was isolated in Kanchanaburi, Thailand in 1979. PfK1 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4) and is reported to be a multidrug-resistant strain. ✖ 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 Pf Plasmodium falciparum P. falciparum (Pf) is one of five protozoan parasite species of the genus Plasmodium that cause malaria in humans. Pf is responsible for the majority of malaria related deaths and is the most prevalent species in sub-Saharan Africa. ✖ 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].