Chromatin regulation in schistosomes and histone modifying enzymes as drug targets
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Publication Date: | 2011 |
Other Authors: | , , , , , , |
Format: | Article |
Language: | eng |
Source: | Memórias do Instituto Oswaldo Cruz |
Download full: | http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0074-02762011000700003 |
Summary: | 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. |
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Chromatin regulation in schistosomes and histone modifying enzymes as drug targetsSchistosoma mansonihistone modifying enzymehistone deacetylaseinhibitordrug targetOnly 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.Instituto Oswaldo Cruz, Ministério da Saúde2011-11-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersiontext/htmlhttp://www.scielo.br/scielo.php?script=sci_arttext&pid=S0074-02762011000700003Memórias do Instituto Oswaldo Cruz v.106 n.7 2011reponame:Memórias do Instituto Oswaldo Cruzinstname:Fundação Oswaldo Cruzinstacron:FIOCRUZ10.1590/S0074-02762011000700003info:eu-repo/semantics/openAccessPierce,Raymond JohnDubois-Abdesselem,FlorenceCaby,StéphanieTrolet,JacquesLancelot,JulienOger,FrédérikBertheaume,NicolasRoger,Emmanueleng2020-04-25T17:51:04Zhttp://www.scielo.br/oai/scielo-oai.php0074-02761678-8060opendoar:null2020-04-26 02:17:52.752Memórias do Instituto Oswaldo Cruz - Fundação Oswaldo Cruztrue |
dc.title.none.fl_str_mv |
Chromatin regulation in schistosomes and histone modifying enzymes as drug targets |
title |
Chromatin regulation in schistosomes and histone modifying enzymes as drug targets |
spellingShingle |
Chromatin regulation in schistosomes and histone modifying enzymes as drug targets Pierce,Raymond John Schistosoma mansoni histone modifying enzyme histone deacetylase inhibitor drug target |
title_short |
Chromatin regulation in schistosomes and histone modifying enzymes as drug targets |
title_full |
Chromatin regulation in schistosomes and histone modifying enzymes as drug targets |
title_fullStr |
Chromatin regulation in schistosomes and histone modifying enzymes as drug targets |
title_full_unstemmed |
Chromatin regulation in schistosomes and histone modifying enzymes as drug targets |
title_sort |
Chromatin regulation in schistosomes and histone modifying enzymes as drug targets |
author |
Pierce,Raymond John |
author_facet |
Pierce,Raymond John Dubois-Abdesselem,Florence Caby,Stéphanie Trolet,Jacques Lancelot,Julien Oger,Frédérik Bertheaume,Nicolas Roger,Emmanuel |
author_role |
author |
author2 |
Dubois-Abdesselem,Florence Caby,Stéphanie Trolet,Jacques Lancelot,Julien Oger,Frédérik Bertheaume,Nicolas Roger,Emmanuel |
author2_role |
author author author author author author author |
dc.contributor.author.fl_str_mv |
Pierce,Raymond John Dubois-Abdesselem,Florence Caby,Stéphanie Trolet,Jacques Lancelot,Julien Oger,Frédérik Bertheaume,Nicolas Roger,Emmanuel |
dc.subject.por.fl_str_mv |
Schistosoma mansoni histone modifying enzyme histone deacetylase inhibitor drug target |
topic |
Schistosoma mansoni histone modifying enzyme histone deacetylase inhibitor drug target |
dc.description.none.fl_txt_mv |
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. |
description |
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. |
publishDate |
2011 |
dc.date.none.fl_str_mv |
2011-11-01 |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0074-02762011000700003 |
url |
http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0074-02762011000700003 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
10.1590/S0074-02762011000700003 |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
text/html |
dc.publisher.none.fl_str_mv |
Instituto Oswaldo Cruz, Ministério da Saúde |
publisher.none.fl_str_mv |
Instituto Oswaldo Cruz, Ministério da Saúde |
dc.source.none.fl_str_mv |
Memórias do Instituto Oswaldo Cruz v.106 n.7 2011 reponame:Memórias do Instituto Oswaldo Cruz instname:Fundação Oswaldo Cruz instacron:FIOCRUZ |
reponame_str |
Memórias do Instituto Oswaldo Cruz |
collection |
Memórias do Instituto Oswaldo Cruz |
instname_str |
Fundação Oswaldo Cruz |
instacron_str |
FIOCRUZ |
institution |
FIOCRUZ |
repository.name.fl_str_mv |
Memórias do Instituto Oswaldo Cruz - Fundação Oswaldo Cruz |
repository.mail.fl_str_mv |
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1669937710024884224 |