Targeting Plasmodium PI(4)K to eliminate malaria

Nature. 2013 Dec 12;504(7479):248-253. doi: 10.1038/nature12782. Epub 2013 Nov 27.

Abstract

Achieving the goal of malaria elimination will depend on targeting Plasmodium pathways essential across all life stages. Here we identify a lipid kinase, phosphatidylinositol-4-OH kinase (PI(4)K), as the target of imidazopyrazines, a new antimalarial compound class that inhibits the intracellular development of multiple Plasmodium species at each stage of infection in the vertebrate host. Imidazopyrazines demonstrate potent preventive, therapeutic, and transmission-blocking activity in rodent malaria models, are active against blood-stage field isolates of the major human pathogens P. falciparum and P. vivax, and inhibit liver-stage hypnozoites in the simian parasite P. cynomolgi. We show that imidazopyrazines exert their effect through inhibitory interaction with the ATP-binding pocket of PI(4)K, altering the intracellular distribution of phosphatidylinositol-4-phosphate. Collectively, our data define PI(4)K as a key Plasmodium vulnerability, opening up new avenues of target-based discovery to identify drugs with an ideal activity profile for the prevention, treatment and elimination of malaria.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • 1-Phosphatidylinositol 4-Kinase / antagonists & inhibitors*
  • 1-Phosphatidylinositol 4-Kinase / chemistry
  • 1-Phosphatidylinositol 4-Kinase / genetics
  • 1-Phosphatidylinositol 4-Kinase / metabolism
  • Adenosine Triphosphate / metabolism
  • Animals
  • Binding Sites
  • Cytokinesis / drug effects
  • Drug Resistance / drug effects
  • Drug Resistance / genetics
  • Fatty Acids / metabolism
  • Female
  • Hepatocytes / parasitology
  • Humans
  • Imidazoles / metabolism
  • Imidazoles / pharmacology
  • Life Cycle Stages / drug effects
  • Macaca mulatta
  • Malaria / drug therapy*
  • Malaria / parasitology*
  • Male
  • Models, Biological
  • Models, Molecular
  • Phosphatidylinositol Phosphates / metabolism
  • Plasmodium / classification
  • Plasmodium / drug effects*
  • Plasmodium / enzymology*
  • Plasmodium / growth & development
  • Pyrazoles / metabolism
  • Pyrazoles / pharmacology
  • Quinoxalines / metabolism
  • Quinoxalines / pharmacology
  • Reproducibility of Results
  • Schizonts / cytology
  • Schizonts / drug effects
  • rab GTP-Binding Proteins / genetics
  • rab GTP-Binding Proteins / metabolism

Substances

  • Fatty Acids
  • Imidazoles
  • Phosphatidylinositol Phosphates
  • Pyrazoles
  • Quinoxalines
  • phosphatidylinositol 4-phosphate
  • Adenosine Triphosphate
  • 1-Phosphatidylinositol 4-Kinase
  • rab11 protein
  • rab GTP-Binding Proteins