Lain S~Westwood NJ, 2008

Pubmed ID 18455128
Title Discovery, in vivo activity, and mechanism of action of a small-molecule p53 activator.
Authors Sonia Lain, Jonathan J Hollick, Johanna Campbell, Oliver D Staples, Maureen Higgins, Mustapha Aoubala, Anna McCarthy, Virginia Appleyard, Karen E Murray, Lee Baker, Alastair Thompson, Joanne Mathers, Stephen J Holland, Michael J R Stark, Georgia Pass, Julie Woods, David P Lane, Nicholas J Westwood
Abstract We have carried out a cell-based screen aimed at discovering small molecules that activate p53 and have the potential to decrease tumor growth. Here, we describe one of our hit compounds, tenovin-1, along with a more water-soluble analog, tenovin-6. Via a yeast genetic screen, biochemical assays, and target validation studies in mammalian cells, we show that tenovins act through inhibition of the protein-deacetylating activities of SirT1 and SirT2, two important members of the sirtuin family. Tenovins are active on mammalian cells at one-digit micromolar concentrations and decrease tumor growth in vivo as single agents. This underscores the utility of these compounds as biological tools for the study of sirtuin function as well as their potential therapeutic interest.
Citation Cancer Cell 2008; 13:454-63

Datasets

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Paper Phenotype Condition Medium Collection Tested mutants Data Details
Lain S~Westwood NJ, 2008 growth (culture turbidity) Tenovin-6 [16.7 uM] YPAD + DMSO [1%] het 6,062 Discrete

Curation history

Data

July 4, 2020 To request.
July 10, 2020 Request sent.
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