Synthesis and biological characterisation of sirtuin inhibitors based on the tenovins

Anna R. McCarthy, Lisa Pirrie, Jonathan J. Hollick, Sebastien Ronseaux, Johanna Campbell, Maureen Higgins, Oliver D. Staples, Fanny Tran, Alexandra M. Z. Slawin, Sonia Lain, Nicholas J. Westwood

Research output: Contribution to journalArticlepeer-review

49 Citations (Scopus)

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. (C) 2012 Elsevier Ltd. All rights reserved.

Original languageEnglish
Pages (from-to)1779-1793
Number of pages15
JournalBioorganic & Medicinal Chemistry
Volume20
Issue number5
DOIs
Publication statusPublished - 1 Mar 2012

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