Chromatin regulation in schistosomes and histone modifying enzymes as drug targets
Mem. Inst. Oswaldo Cruz
;
106(7): 794-801, Nov. 2011. ilus
Article
in English
| LILACS
| ID: lil-606641
ABSTRACT
Only one drug is currently available for the treatment and control of schistosomiasis and the increasing risk of selecting strains of schistosome that are resistant to praziquantel means that the development of new drugs is urgent. With this objective we have chosen to target the enzymes modifying histones and in particular the histone acetyltransferases and histone deacetylases (HDAC). Inhibitors of HDACs (HDACi) are under intense study as potential anti-cancer drugs and act via the induction of cell cycle arrest and/or apoptosis. Schistosomes like other parasites can be considered as similar to tumours in that they maintain an intense metabolic activity and rate of cell division that is outside the control of the host. We have shown that HDACi can induce apoptosis and death of schistosomes maintained in culture and have set up a consortium (Schistosome Epigenetics Targets, Regulation, New Drugs) funded by the European Commission with the aim of developing inhibitors specific for schistosome histone modifying enzymes as novel lead compounds for drug development.
Full text:
Available
Index:
LILACS (Americas)
Main subject:
Schistosoma
/
Chromatin
/
Enzyme Inhibitors
/
Histone Acetyltransferases
/
Histone Deacetylases
Limits:
Animals
Language:
English
Journal:
Mem. Inst. Oswaldo Cruz
Journal subject:
Tropical Medicine
/
Parasitology
Year:
2011
Type:
Article
Affiliation country:
France
Institution/Affiliation country:
Institut Pasteur de Lille/FR
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