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dc.contributor.authorTintoré, Maríaes_ES
dc.contributor.authorEritja Casadellà, Ramónes_ES
dc.contributor.authorGrijalvo, Santiagoes_ES
dc.contributor.authorFàbrega, Carmees_ES
dc.date.accessioned2016-03-07T10:44:29Z-
dc.date.available2016-03-07T10:44:29Z-
dc.date.issued2015-11-15-
dc.identifier.citationBioorganic and Medicinal Chemistry Letterses_ES
dc.identifier.urihttp://hdl.handle.net/10261/129819-
dc.description.abstractO6-alkylguanine-DNA-alkyltransferase (hAGT) activity provides resistance to cancer chemotherapeutic agents and its inhibition enhances chemotherapy. We herein present the development of a novel fluorescence assay for the detection of hAGT activity. We designed a dsDNA sequence containing a fluorophore-quencher pair, where the fluorophore was attached to an O6-benzylguanine. This precursor was synthesized using the Mitsunobu reaction to introduce the benzyl group. The alkyl-fluorophore group is transferred to the active site during the dealkylation, producing an increase in fluorescence which is correlated to hAGT activity. This assay can be used for the evaluation of potential inhibitors of hAGT in a straightforward manner.es_ES
dc.description.sponsorshipThe Communities MULTIFUN (contract NMP4-LA-2011-262943), Spanish Healthcare Research Fund (grant PI06/1250) and Spanish Ministry of Economy and Competitiveness (grants CTQ-2010-20541-C03-03 and CTQ2014-52588-R) are acknowledged for financialsupport. M.T. was supported by a pre-doctoral fellowship (FPI) from MINECO. C.F is grateful to TV3 Marato 2012 for a research contract.es_ES
dc.language.isoenges_ES
dc.publisherElsevieres_ES
dc.relationinfo:eu-repo/grantAgreement/MINECO/Plan Estatal de Investigación Científica y Técnica y de Innovación 2013-2016/CTQ2014-52588-Res_ES
dc.relationinfo:eu-repo/grantAgreemeent/EC/FP7/262943-
dc.relation.isversionofPostprintes_ES
dc.rightsopenAccessen_EN
dc.subjectDNA repaires_ES
dc.subjectFluorescencees_ES
dc.subjectMitsunobues_ES
dc.subjectO6-alkylguanine-DNA alkyltransferasees_ES
dc.subjectOligonucleotide synthesises_ES
dc.titleSynthesis of oligonucleotides carrying fluorescently labelled O6-alkylguanine for measuring hAGT activityes_ES
dc.typeartículoes_ES
dc.identifier.doi10.1016/j.bmcl.2015.09.065-
dc.description.peerreviewedPeer reviewedes_ES
dc.relation.publisherversionhttp://www.sciencedirect.com/science/article/pii/S0960894X15300998es_ES
dc.embargo.terms2017-11-16es_ES
dc.rights.licensehttps://www.elsevier.com/journals/bioorganic-and-medicinal-chemistry-letters/0960-894X/open-access-optionses_ES
dc.contributor.funderMinisterio de Economía y Competitividad (España)es_ES
dc.relation.csices_ES
dc.identifier.funderhttp://dx.doi.org/10.13039/501100003329es_ES
dc.type.coarhttp://purl.org/coar/resource_type/c_6501es_ES
item.openairetypeartículo-
item.cerifentitytypePublications-
item.fulltextWith Fulltext-
item.languageiso639-1en-
item.openairecristypehttp://purl.org/coar/resource_type/c_18cf-
item.grantfulltextopen-
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