Please use this identifier to cite or link to this item:
http://hdl.handle.net/2445/173502
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DC Field | Value | Language |
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dc.contributor.author | Turrado, Carlos | - |
dc.contributor.author | Puig i Miquel, Teresa | - |
dc.contributor.author | García-Cárceles, Javier | - |
dc.contributor.author | Artola Pino, Marta | - |
dc.contributor.author | Benhamú, Bellinda | - |
dc.contributor.author | Ortega-Gutiérrez, Silvia | - |
dc.contributor.author | Relat Pardo, Joana | - |
dc.contributor.author | Oliveras Serrat, Glòria | - |
dc.contributor.author | Blancafort, Adriana | - |
dc.contributor.author | Haro Bautista, Diego | - |
dc.contributor.author | Marrero González, Pedro F. | - |
dc.contributor.author | Colomer Bosch, Ramón | - |
dc.contributor.author | López-Rodríguez, María Luz | - |
dc.date.accessioned | 2021-01-28T14:10:48Z | - |
dc.date.available | 2021-01-28T14:10:48Z | - |
dc.date.issued | 2012-05-04 | - |
dc.identifier.issn | 0022-2623 | - |
dc.identifier.uri | http://hdl.handle.net/2445/173502 | - |
dc.description.abstract | Fatty acid synthase (FASN) is a lipogenic enzyme that is highly expressed in different human cancers. Here we report the development of a new series of polyphenolic compounds 5-30 that have been evaluated for their cytotoxic capacity in SK-Br3 cells, a human breast cancer cell line with high FASN expression. The compounds with an IC50 < 50 M have been tested for their ability to inhibit FASN activity. Among them, derivative 30 blocks the 90% of FASN activity at low concentration (4 M), is highly cytotoxic in a broad panel of tumor cells, induces apoptosis, and blocks the activation of HER2, AKT and ERK pathways. Remarkably, 30 does not activate carnitine palmitoyltransferase-1 (CPT-1) nor induces in mice weight loss, which are the main drawbacks of other previously described FASN inhibitors. Thus, FASN inhibitor 30 may aid the validation of this enzyme as a therapeutic target for the treatment of cancer. | - |
dc.format.extent | 11 p. | - |
dc.format.mimetype | application/pdf | - |
dc.language.iso | eng | - |
dc.publisher | American Chemical Society | - |
dc.relation.isformatof | Versió postprint del document publicat a: https://doi.org/10.1021/jm2016045 | - |
dc.relation.ispartof | Journal of Medicinal Chemistry, 2012, vol. 55, num. 11, p. 5013-5023 | - |
dc.relation.uri | https://doi.org/10.1021/jm2016045 | - |
dc.rights | (c) American Chemical Society , 2012 | - |
dc.source | Articles publicats en revistes (Nutrició, Ciències de l'Alimentació i Gastronomia) | - |
dc.subject.classification | Àcids grassos | - |
dc.subject.classification | Metabolisme | - |
dc.subject.classification | Inhibidors enzimàtics | - |
dc.subject.other | Fatty acids | - |
dc.subject.other | Metabolism | - |
dc.subject.other | Enzyme inhibitors | - |
dc.title | New synthetic inhibitors of fatty acid synthase with anticancer activity | - |
dc.type | info:eu-repo/semantics/article | - |
dc.type | info:eu-repo/semantics/acceptedVersion | - |
dc.identifier.idgrec | 613827 | - |
dc.date.updated | 2021-01-28T14:10:49Z | - |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | - |
Appears in Collections: | Articles publicats en revistes (Nutrició, Ciències de l'Alimentació i Gastronomia) |
Files in This Item:
File | Description | Size | Format | |
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613827.pdf | 962.66 kB | Adobe PDF | View/Open |
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