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epigenetic inhibitors

Not Open Access | Activity of epigenetic inhibitors against Plasmodium falciparum asexual and sexual blood stages

May 6, 2020 - 16:02 -- NOT Open Access
Author(s): 
Vanheer LN, Zhang H, Lin G, Kafsack BFC
Reference: 
Antimicrob Agents Chemother. 2020 May 4. pii: AAC.02523-19

Earlier genetic and inhibitor studies have shown that epigenetic regulation of gene expression is critical for malaria parasite survival in multiple life stages and a promising target for new anti-malarials.

Epigenetic inhibitors target multiple stages of Plasmodium falciparum parasites

February 14, 2020 - 17:04 -- Open Access
Author(s): 
Coetzee N, von Grüning H, Opperman D, van der Watt M, Reader J, Birkholtz LM
Reference: 
Sci Rep. 2020 Feb 11; 10(1):2355

The epigenome of the malaria parasite, Plasmodium falciparum, is associated with regulation of various essential processes in the parasite including control of proliferation during asexual development as well as control of sexual differentiation. The unusual nature of the epigenome has prompted investigations into the potential to target epigenetic modulators with novel chemotypes. Here, we explored the diversity within a library of 95 compounds, active against various epigenetic modifiers in cancerous cells, for activity against multiple stages of P. falciparum development.

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