期刊
FUTURE MEDICINAL CHEMISTRY
卷 7, 期 6, 页码 783-800出版社
FUTURE SCI LTD
DOI: 10.4155/FMC.15.25
关键词
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资金
- European Union [241865, 602080]
- Centre National de la Recherche Scientifique (CNRS)
- Institut National de la Sante et de la Recherche Medicale (INSERM)
- Universite de Strasbourg and the Universite de Lille 2
- French Infrastructure for Integrated Structural Biology (FRISBI) [ANR-10-INSB-05-01]
- European Strategy Forum on Research Infrastructures (ESFRI)
- Deutsche Forschungsgemeinschaft (DFG)
- CNPq [309312/2012-4, 403049/20121]
- FAPEMIG [PPM-00439-10]
Schistosomes, like many eukaryotic pathogens, typically display morphologically distinct stages during their life cycles. Epigenetic mechanisms underlie the pathogens' morphological transformations, and the targeting of epigenetics-driven cellular programs therefore represents an Achilles' heel of parasites. To speed up the search for new antiparasitic agents, drugs validated for other diseases can be rationally optimized into antiparasitic therapeutics. Specifically, zinc-dependent histone deacetylases (HDACs) are the most explored targets for epigenetic therapies, notably for anticancer treatments. This review focuses on the development of drug-leads inhibiting HDACs from schistosomes. More precisely, current progress on Schistosoma mansoni HDAC8 (smHDAC8) provided a proof of concept that targeting epigenetic enzymes is a valid approach to treat diseases caused by schistosomes, and possibly other eukaryotic pathogens.
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