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dc.contributor.authorTurrado, Carlos-
dc.contributor.authorPuig i Miquel, Teresa-
dc.contributor.authorGarcía-Cárceles, Javier-
dc.contributor.authorArtola Pino, Marta-
dc.contributor.authorBenhamú, Bellinda-
dc.contributor.authorOrtega-Gutiérrez, Silvia-
dc.contributor.authorRelat Pardo, Joana-
dc.contributor.authorOliveras Serrat, Glòria-
dc.contributor.authorBlancafort, Adriana-
dc.contributor.authorHaro Bautista, Diego-
dc.contributor.authorMarrero González, Pedro F.-
dc.contributor.authorColomer Bosch, Ramón-
dc.contributor.authorLópez-Rodríguez, María Luz-
dc.description.abstractFatty 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.extent11 p.-
dc.publisherAmerican Chemical Society-
dc.relation.isformatofVersió postprint del document publicat a:
dc.relation.ispartofJournal of Medicinal Chemistry, 2012, vol. 55, num. 11, p. 5013-5023-
dc.rights(c) American Chemical Society , 2012-
dc.sourceArticles publicats en revistes (Nutrició, Ciències de l'Alimentació i Gastronomia)-
dc.subject.classificationÀcids grassos-
dc.subject.classificationInhibidors enzimàtics-
dc.subject.otherFatty acids-
dc.subject.otherEnzyme inhibitors-
dc.titleNew synthetic inhibitors of fatty acid synthase with anticancer activity-
Appears in Collections:Articles publicats en revistes (Nutrició, Ciències de l'Alimentació i Gastronomia)

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