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  • The Salerno: new selective inhibitor of sirtuins with proapoptotic activity

    str49Sirtuins (SIRT), protein family of histone deacetylases (HDAC) are involved in processes such as longevity, cancer, gene regulation, energy homeostasis and apoptosis.Inhibitors of sirtuins have antitumor properties, but so far no known inhibitor, such small molecule that is capable of discriminating between different members of the family of sirtuins.

    The study, conducted by the groups of Dr. Fraga (Cancer Epigenetics Laboratory of National Cancer Research Center, CNIO) and Dr. Esteller (Program for Epigenetics and Cancer Biology at the Catalan Institute of Oncology, ICO), describes the design, synthesis and biological activity of Salerno, a new and potent inhibitor in vitro of sirtuins SIRT1 and SIRT2.

    The Salerno is designed based on sirtinol, one of inhibitors of sirtuins in greater antitumor inhibitory capacity. This regioisomer of sirtinol produces a massive induction of apoptosis without affecting the cell cycle, specific for tumor cells and dose-dependent. After intraperitoneal injection of the compound in mice (nude mice) no apparent toxicity in vivo. The researchers state that the apoptotic effect of Salerno is due in part to the revival of pro-apoptotic gene that epigenetically, are repressed by Sirt1 exclusively in cancer cells.

    This paper highlights the importance of Salerno as a new antitumor drug candidate and at the same time, provides evidence at the molecular level of how Sirt1 is involved in tumorigenesis in humans.

    Published on November 10, 2012 · Filed under: Bioscience; Tagged as: , , , , , ,
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