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Plasmodium falciparum hydroxymethyldihydropterin pyrophosphokinase-dihydropteroate synthase

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Target not currently curated in GtoImmuPdb

Malaria Pharmacology Ligand  Target has curated data in GtoMPdb

Target id: 3065

Nomenclature: Plasmodium falciparum hydroxymethyldihydropterin pyrophosphokinase-dihydropteroate synthase

Abbreviated Name: PfPPPK-DHPS

Family: Folate biosynthesis enzymes

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Plasmodium falciparum 3D7 - 706 PPPK-DHPS hydroxymethyldihydropterin pyrophosphokinase-dihydropteroate synthase
Previous and Unofficial Names Click here for help
PPPK-DHPS | hydroxymethyldihydropterin pyrophosphokinase-dihydropteroate synthase
Database Links Click here for help
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Inhibitors
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Ligand Sp. Action Value Parameter Reference
dapsone Small molecule or natural product Approved drug Pf Inhibition 5.2 pKi 3
pKi 5.2 (Ki 6x10-6 M) [3]
Description: Enzyme inhibition assay.
Whole Organism Assay Data Linked to This Target
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Ligand Sp. Assay description Type Action Value Parameter Reference
sulfadoxine Small molecule or natural product Approved drug PfHB3 Parasite growth inhibition assay - - 8.4 pIC50 2
pIC50 8.4 (IC50 4x10-9 M) [3H]-hypoxanthine incorporation [2]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
sulfadoxine Small molecule or natural product Approved drug Pf3D7 Parasite growth inhibition assay - - 7.1 pIC50 2
pIC50 7.1 (IC50 7.3x10-8 M) [3H]-hypoxanthine incorporation [2]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
sulfadoxine Small molecule or natural product Approved drug PfK1 Parasite growth inhibition assay - - 6.7 pIC50 2
pIC50 6.7 (IC50 2.23x10-7 M) [3H]-hypoxanthine incorporation [2]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
sulfadoxine Small molecule or natural product Approved drug PfDd2 Parasite growth inhibition assay - - 5.4 pIC50 2
pIC50 5.4 (IC50 3.97x10-6 M) [3H]-hypoxanthine incorporation [2]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Malaria Pharmacology Comments
The Plasmodium enzyme hydroxymethyldihydropterin pyrophosphokinase-dihydropteroate synthase (PfPPPK-DHPS) is a bifunctional protein involved in the folate biosynthesis pathway and in the mechanism of action of the sulfonamide group of drugs [1].

References

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1. Triglia T, Cowman AF. (1994) Primary structure and expression of the dihydropteroate synthetase gene of Plasmodium falciparum. Proc Natl Acad Sci USA, 91 (15): 7149-53. [PMID:8041761]

2. Wang P, Read M, Sims PF, Hyde JE. (1997) Sulfadoxine resistance in the human malaria parasite Plasmodium falciparum is determined by mutations in dihydropteroate synthetase and an additional factor associated with folate utilization. Mol Microbiol, 23 (5): 979-86. [PMID:9076734]

3. Zhang Y, Meshnick SR. (1991) Inhibition of Plasmodium falciparum dihydropteroate synthetase and growth in vitro by sulfa drugs. Antimicrob Agents Chemother, 35 (2): 267-71. [PMID:2024960]

How to cite this page

Folate biosynthesis enzymes: Plasmodium falciparum hydroxymethyldihydropterin pyrophosphokinase-dihydropteroate synthase. Last modified on 01/02/2021. Accessed on 22/09/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=3065.