Utilize este identificador para referenciar este registo: https://hdl.handle.net/1822/62298

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dc.contributor.authorDuarte, Dianapor
dc.contributor.authorFraga, Alexandra Gabrielpor
dc.contributor.authorPedrosa, Jorgepor
dc.contributor.authorMartel, Fátimapor
dc.contributor.authorVale, Nunopor
dc.date.accessioned2019-11-21T11:32:33Z-
dc.date.available2020-10-05T06:00:17Z-
dc.date.issued2019-10-05-
dc.identifier.issn0014-2999-
dc.identifier.urihttps://hdl.handle.net/1822/62298-
dc.description.abstractCancer treatment is one of the major fields of interest for the scientific community. Investment in cancer research is costly but essential to provide patients with more effective and safe treatments. In this project, we describe the synthesis and characterization of new thiazole derivatives coupled to CPP2, a cell-penetrating peptide (CPP) reported for colon cancer cells. Using a human adenocarcinoma-derived cell line (Caco-2), these new CPPs were evaluated for antiproliferative (3H-thymidine incorporation) and cytotoxic effect (extracellular lactate dehydrogenase activity). One of these derivatives, the BTZCA thiazole compound and its peptide-conjugated (BTZCA-CPP2) also showed the ability to decrease tumour cell viability and proliferation, with potential cytotoxic effect against human breast cancer MCF-7 cells. Then, cytotoxicity studies were developed against J774, L929 and THP1 cell lines and this new family showed no significant cytotoxicity, when compared to their counterparts alone (BTZCA and CPP2). The use of smaller CPP conjugated with this family of derivatives can be also considered in future for the development of new drugs to cancer therapy.por
dc.description.sponsorshipThis work was financed by FEDER - Fundo Europeu de Desenvolvimento Regional funds through the COMPETE 2020 - Operacional Programme for Competitiveness and Internationalisation (POCI), Portugal 2020, and by Portuguese funds through FCT - Fundação para a Ciência e a Tecnologia, in the framework of the project “Institute for Research and Innovation in Health Sciences” (POCI-01- 0145-FEDER-007274)." This work was also financed by FCT and FEDER (European Union), through project IF/00092/2014/CP1255/CT0004. NV thanks FCT by IF position, DQB-Faculty of Sciences from University of Porto, for support in peptide synthesis, and Fundação Manuel António da Mota by support Nuno Vale Lab. DD thanks FCT for PhD grant with ref. SFRH/BD/140734/2018. AGF and JP were involved in the cytotoxicity assays, which were developed within the scope of the projects NORTE-01-0145-FEDER-000013 and NORTE-01-0145-FEDER000023, supported by the Northern Portugal Regional Operational Programme (NORTE 2020), under the Portugal 2020 Partnership Agreement through FEDER. This work was also financed through the Competitiveness Factors Operational Programme (COMPETE) and by national funds, through FCT, under the scope of the project POCI-01- 0145-FEDER-007038. AGF would also like to acknowledge FCT for the post-doc fellow SFRH/BPD/112903/2015. The contents of this report are solely the responsibility of the authors and do not necessarily represent the official views of the FCT or FMAM.por
dc.language.isoengpor
dc.publisherElsevier 1por
dc.rightsopenAccesspor
dc.subjectCell-penetrating peptidepor
dc.subjectCPP2por
dc.subjectThiazolepor
dc.subjectMCF-7por
dc.subjectCaco-2por
dc.subjectCell-penetrating peptidespor
dc.titleIncreasing the potential of cell-penetrating peptides for cancer therapy using a new pentagonal scaffoldpor
dc.typearticlepor
dc.peerreviewedyespor
oaire.citationStartPage172554(1)por
oaire.citationEndPage172554(11)por
oaire.citationVolume860por
dc.identifier.eissn1879-0712-
dc.identifier.doi10.1016/j.ejphar.2019.172554por
dc.identifier.pmid31326378por
dc.subject.wosScience & Technologypor
sdum.journalEuropean Journal of Pharmacologypor
Aparece nas coleções:ICVS - Artigos em revistas internacionais / Papers in international journals

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