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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??M for 28% of compounds against asexual blood stages and early gametocytes, of which a third retained ?90% inhibition at 1??M.

SUBMITTER: Vanheer LN 

PROVIDER: S-EPMC7318029 | biostudies-literature | 2020 Jun

REPOSITORIES: biostudies-literature

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

Vanheer Leen N LN   Zhang Hao H   Lin Gang G   Kafsack Björn F C BFC  

Antimicrobial agents and chemotherapy 20200623 7


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 <i>Plasmodium falciparum</i> 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. ...[more]

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