Synthesis and biological characterisation of sirtuin inhibitors based on the tenovins |
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| Authors: | McCarthy Anna R Pirrie Lisa Hollick Jonathan J Ronseaux Sebastien Campbell Johanna Higgins Maureen Staples Oliver D Tran Fanny Slawin Alexandra M Z Lain Sonia Westwood Nicholas J |
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| Institution: | School of Chemistry and Biomedical Sciences Research Complex, University of St. Andrews, North Haugh, St. Andrews, Fife, UK. |
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| Abstract: | The tenovins are small molecule inhibitors of the NAD(+)-dependent family of protein deacetylases known as the sirtuins. There remains considerable interest in inhibitors of this enzyme family due to possible applications in both cancer and neurodegenerative disease therapy. Through the synthesis of novel tenovin analogues, further insights into the structural requirements for activity against the sirtuins in vitro are provided. In addition, the activity of one of the analogues in cells led to an improved understanding of the function of SirT1 in cells. |
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