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

ABSTRACT

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.