Gene and Protein Information
Species	TM	AA	Chromosomal Location	Gene Symbol	Gene Name	Reference
Plasmodium falciparum 3D7	-	376		FPPS/GGPPS	bifunctional farnesyl/geranylgeranyl diphosphate synthase

Previous and Unofficial Names

FPPS/GGPPS | Pf3D7_11_v3:1,104,154..1,107,028(-) | PF11_0295

Database Links
Alphafold	Q8II79 (Pf3D7)
PlasmoDB	PF3D7_1128400 (Pf3D7)
UniProtKB	Q8II79 (Pf3D7)

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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 AIM-1290 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 5.7 pIC50 3 ⤷ pIC50 5.7 (IC50 1.94x10-6 M) PfGGPPS enzymatic activity [3]

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 MMV019313 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. ✖ - - 6.7 pEC50 1 ⤷ pEC50 6.7 (EC50 1.8x10-7 M) [1] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont) MMV019313 PfW2 Plasmodium falciparum W2 P. falciparum strain W2 (PfW2) was cloned from the Indochina III/CDC isolate, originally derived from a Laotian patient who failed chloroquine therapy. PfW2 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4) and is reported to be resistant to chloroquine and susceptible to mefloquine. ✖ - - 6.6 pEC50 1 ⤷ pEC50 6.6 (EC50 2.7x10-7 M) [1] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont) AIM-1290 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. ✖ Parasite growth inhibition assay - - 7.1 pIC50 3 ⤷ pIC50 7.1 (IC50 7.4x10-8 M) [3] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)

Malaria Pharmacology Comments

The Plasmodium enzyme bifunctional farnesyl/geranylgeranyl diphosphate (PfFPPS/GGPPS) is an essential branchpoint enzyme in isoprenoid biosynthesis in the parasite [2]. Bisphosphonate drugs, that inhibit Human FDPS and GGPS1, demonstrate poor bioavailability and selectivity for PfFPPS/GGPPS leading to the identification and development of more selective compounds [1,3].