Synthesis and biological characterisation of sirtuin inhibitors based on the tenovins.
| Autor: | McCarthy AR; School of Chemistry and Biomedical Sciences Research Complex, University of St. Andrews, North Haugh, St. Andrews, Fife, UK., Pirrie L, Hollick JJ, Ronseaux S, Campbell J, Higgins M, Staples OD, Tran F, Slawin AM, Lain S, Westwood NJ |
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| Jazyk: | angličtina |
| Zdroj: | Bioorganic & medicinal chemistry [Bioorg Med Chem] 2012 Mar 01; Vol. 20 (5), pp. 1779-93. Date of Electronic Publication: 2012 Jan 12. |
| DOI: | 10.1016/j.bmc.2012.01.001 |
| Abstrakt: | 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. (Copyright © 2012 Elsevier Ltd. All rights reserved.) |
| Databáze: | MEDLINE |
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