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New synthetic inhibitors of fatty acid synthase with anticancer activity
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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.
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TURRADO, Carlos, PUIG I MIQUEL, Teresa, GARCÍA-CÁRCELES, Javier, ARTOLA PINO, Marta, BENHAMÚ, Bellinda, ORTEGA-GUTIÉRREZ, Silvia, RELAT PARDO, Joana, OLIVERAS SERRAT, Glòria, BLANCAFORT, Adriana, HARO BAUTISTA, Diego, MARRERO GONZÁLEZ, Pedro f., COLOMER BOSCH, Ramón, LÓPEZ-RODRÍGUEZ, María luz. New synthetic inhibitors of fatty acid synthase with anticancer activity. _Journal of Medicinal Chemistry_. 2012. Vol. 55, núm. 11, pàgs. 5013-5023. [consulta: 21 de gener de 2026]. ISSN: 0022-2623. [Disponible a: https://hdl.handle.net/2445/173502]