The anticancer agent ellipticine unwinds DNA by intercalative binding in an orientation parallel to base pairs

Ellipticine is a natural plant product that has been found to be a powerful anticancer drug. Although still unclear, its mechanism of action is considered to be mainly based on DNA intercalation and/or the inhibition of topoisomerase II. Many experimental data suggest an intercalation based on stack...

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Authors: Canals, Albert, Purciolas, Mònica, Aymamí, Joan, Coll, Miquel
Format: article
Publication Date:2005
Country:España
Institution:Consejo Superior de Investigaciones Científicas (CSIC)
Repository:DIGITAL.CSIC. Repositorio Institucional del CSIC
OAI Identifier:oai:digital.csic.es:10261/108793
Online Access:http://hdl.handle.net/10261/108793
Access Level:Open access
Keyword:Anticancer drugs
intercalating agent
ellipticine derivative
ellipticine
DNA
Antineoplastic agents
DNA binding
drug design
intercalators
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network_acronym_str ES
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spelling The anticancer agent ellipticine unwinds DNA by intercalative binding in an orientation parallel to base pairsCanals, AlbertPurciolas, MònicaAymamí, JoanColl, MiquelAnticancer drugsintercalating agentellipticine derivativeellipticineDNAAntineoplastic agentsDNA bindingdrug designintercalatorsellipticineEllipticine is a natural plant product that has been found to be a powerful anticancer drug. Although still unclear, its mechanism of action is considered to be mainly based on DNA intercalation and/or the inhibition of topoisomerase II. Many experimental data suggest an intercalation based on stacking interactions along the major base-pair axis, but alternative binding modes have been proposed, in particular for ellipticine derivatives. The 1.5 Å resolution structure of ellipticine complexed to a 6 bp oligonucleotide unveils its mode of binding and enables a detailed analysis of the distorting effects of the drug on the DNA. © 2005 International Union of Crystallography - all rights reserved.This work was supported by the Ministerio de Educación y Ciencia de España (grants BIO2002-03964 and GEN2003-20642-CO9-01) and by the Generalitat de Catalunya (grant SGR2001-00346)Peer ReviewedBlackwell Publishing2014201420052014info:eu-repo/semantics/articlehttp://purl.org/coar/resource_type/c_6501http://hdl.handle.net/10261/108793reponame:DIGITAL.CSIC. Repositorio Institucional del CSICinstname:Consejo Superior de Investigaciones Científicas (CSIC)Ingléshttp://dx.doi.org/10.1107/S0907444905015404info:eu-repo/semantics/openAccessoai:digital.csic.es:10261/1087932026-05-22T06:33:51Z
dc.title.none.fl_str_mv The anticancer agent ellipticine unwinds DNA by intercalative binding in an orientation parallel to base pairs
title The anticancer agent ellipticine unwinds DNA by intercalative binding in an orientation parallel to base pairs
spellingShingle The anticancer agent ellipticine unwinds DNA by intercalative binding in an orientation parallel to base pairs
Canals, Albert
Anticancer drugs
intercalating agent
ellipticine derivative
ellipticine
DNA
Antineoplastic agents
DNA binding
drug design
intercalators
ellipticine
title_short The anticancer agent ellipticine unwinds DNA by intercalative binding in an orientation parallel to base pairs
title_full The anticancer agent ellipticine unwinds DNA by intercalative binding in an orientation parallel to base pairs
title_fullStr The anticancer agent ellipticine unwinds DNA by intercalative binding in an orientation parallel to base pairs
title_full_unstemmed The anticancer agent ellipticine unwinds DNA by intercalative binding in an orientation parallel to base pairs
title_sort The anticancer agent ellipticine unwinds DNA by intercalative binding in an orientation parallel to base pairs
dc.creator.none.fl_str_mv Canals, Albert
Purciolas, Mònica
Aymamí, Joan
Coll, Miquel
author Canals, Albert
author_facet Canals, Albert
Purciolas, Mònica
Aymamí, Joan
Coll, Miquel
author_role author
author2 Purciolas, Mònica
Aymamí, Joan
Coll, Miquel
author2_role author
author
author
dc.subject.none.fl_str_mv Anticancer drugs
intercalating agent
ellipticine derivative
ellipticine
DNA
Antineoplastic agents
DNA binding
drug design
intercalators
ellipticine
topic Anticancer drugs
intercalating agent
ellipticine derivative
ellipticine
DNA
Antineoplastic agents
DNA binding
drug design
intercalators
ellipticine
description Ellipticine is a natural plant product that has been found to be a powerful anticancer drug. Although still unclear, its mechanism of action is considered to be mainly based on DNA intercalation and/or the inhibition of topoisomerase II. Many experimental data suggest an intercalation based on stacking interactions along the major base-pair axis, but alternative binding modes have been proposed, in particular for ellipticine derivatives. The 1.5 Å resolution structure of ellipticine complexed to a 6 bp oligonucleotide unveils its mode of binding and enables a detailed analysis of the distorting effects of the drug on the DNA. © 2005 International Union of Crystallography - all rights reserved.
publishDate 2005
dc.date.none.fl_str_mv 2005
2014
2014
2014
dc.type.none.fl_str_mv info:eu-repo/semantics/article
http://purl.org/coar/resource_type/c_6501
format article
dc.identifier.none.fl_str_mv http://hdl.handle.net/10261/108793
url http://hdl.handle.net/10261/108793
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv http://dx.doi.org/10.1107/S0907444905015404
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.publisher.none.fl_str_mv Blackwell Publishing
publisher.none.fl_str_mv Blackwell Publishing
dc.source.none.fl_str_mv reponame:DIGITAL.CSIC. Repositorio Institucional del CSIC
instname:Consejo Superior de Investigaciones Científicas (CSIC)
instname_str Consejo Superior de Investigaciones Científicas (CSIC)
reponame_str DIGITAL.CSIC. Repositorio Institucional del CSIC
collection DIGITAL.CSIC. Repositorio Institucional del CSIC
repository.name.fl_str_mv
repository.mail.fl_str_mv
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score 15,812429

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