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Title: New synthetic inhibitors of fatty acid synthase with anticancer activity
Author: 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
Keywords: Àcids grassos
Inhibidors enzimàtics
Fatty acids
Enzyme inhibitors
Issue Date: 4-May-2012
Publisher: American Chemical Society
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.
Note: Versió postprint del document publicat a:
It is part of: Journal of Medicinal Chemistry, 2012, vol. 55, num. 11, p. 5013-5023
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ISSN: 0022-2623
Appears in Collections:Articles publicats en revistes (Nutrició, Ciències de l'Alimentació i Gastronomia)

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