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Updated: May 22, 2026
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Toxicological Assays for Testing Effects of an Epigenetic Drug on Development, Fecundity and Survivorship of Malaria Mosquitoes
Published on: January 16, 2015
Targeting schistosome histone modifying enzymes for drug development
Raymond J Pierce1, Florence Dubois-Abdesselem, Julien Lancelot
1CIIL, Institut Pasteur de Lille, F-59019 Lille, France. raymond.pierce@pasteur-lille.fr
Current Pharmaceutical Design
|May 22, 2012
Summary
Histone modifying enzymes (HMEs) are promising targets for new schistosomiasis drugs. Inhibiting these enzymes, like histone deacetylase 8, can kill schistosome parasites, offering alternatives to praziquantel.
Area of Science:
- Parasitology
- Drug Discovery
- Molecular Biology
Background:
- Schistosomiasis treatment relies solely on praziquantel.
- Histone modifying enzymes (HMEs) are validated anticancer targets.
- Schistosome genome sequencing enables identification of HME targets.
Purpose of the Study:
- To identify and validate schistosome HMEs as drug targets.
- To develop novel therapeutics against schistosomiasis.
- To explore epigenetic regulation in schistosomes.
Main Methods:
- Phylogenetic screening of HME classes.
- High-throughput and in silico screening of HME targets.
- Inhibitor screening against Schistosoma mansoni and Schistosoma japonicum.
Main Results:
- Identified schistosome histone acetyltransferases, deacetylases, methyltransferases, and demethylases.
- Class I histone deacetylase 8 (SmHDAC8) shows catalytic site differences from human HDAC8, enabling specific inhibitor development.
- Inhibitors targeting various HME classes induced apoptosis and death in schistosome parasites in vitro.
Conclusions:
- HMEs are viable drug targets for schistosomiasis.
- Targeting SmHDAC8 specifically is a promising strategy.
- Broader inhibition of HME classes also demonstrates therapeutic potential.
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