2026-04-17T04:25:02Zhttps://recercat.cat/oai/request

oai:recercat.cat:2445/1735022025-12-05T14:54:21Zcom_2072_1057col_2072_478917col_2072_478924

00925njm 22002777a 4500 dc Turrado, Carlos author Puig i Miquel, Teresa author García-Cárceles, Javier author Artola Pino, Marta author Benhamú, Bellinda author Ortega-Gutiérrez, Silvia author Relat Pardo, Joana author Oliveras Serrat, Glòria author Blancafort, Adriana author Haro Bautista, Diego author Marrero González, Pedro F. author Colomer Bosch, Ramón author López-Rodríguez, María Luz author 2021-01-28T14:10:48Z 2021-01-28T14:10:48Z 2012-05-04 2021-01-28T14:10:49Z 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. Àcids grassos Metabolisme Inhibidors enzimàtics Fatty acids Metabolism Enzyme inhibitors New synthetic inhibitors of fatty acid synthase with anticancer activity