Activity of Epigenetic Inhibitors against Plasmodium falciparum Asexual and Sexual Blood Stages

Antimicrob Agents Chemother. 2020 Jun 23;64(7):e02523-19. doi: 10.1128/AAC.02523-19. Print 2020 Jun 23.


Earlier genetic and inhibitor studies showed that epigenetic regulation of gene expression is critical for malaria parasite survival in multiple life stages and a promising target for new antimalarials. We therefore evaluated the activity of 350 diverse epigenetic inhibitors against multiple stages of Plasmodium falciparum We observed ≥90% inhibition at 10 μM for 28% of compounds against asexual blood stages and early gametocytes, of which a third retained ≥90% inhibition at 1 μM.

Keywords: Plasmodium falciparum; antimalarial agents; drug screening; epigenetic inhibitors; malaria; small-molecule screen.

Publication types

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

MeSH terms

  • Antimalarials* / pharmacology
  • Antimalarials* / therapeutic use
  • Epigenesis, Genetic
  • Humans
  • Malaria, Falciparum* / drug therapy
  • Plasmodium falciparum / genetics


  • Antimalarials