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Discovery, in vivo activity, and mechanism of action of a small-molecule p53 activator
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dc.contributor.author | Lain, Sonia | |
dc.contributor.author | Hollick, Jonathan J. | |
dc.contributor.author | Campbell, Johanna | |
dc.contributor.author | Staples, Oliver D. | |
dc.contributor.author | Higgins, Maureen | |
dc.contributor.author | Aoubala, Mustapha | |
dc.contributor.author | McCarthy, Anna | |
dc.contributor.author | Appleyard, Virginia | |
dc.contributor.author | Murray, Karen E. | |
dc.contributor.author | Baker, Lee | |
dc.contributor.author | Thompson, Alastair | |
dc.contributor.author | Mathers, Joanne | |
dc.contributor.author | Holland, Stephen J. | |
dc.contributor.author | Stark, Michael J. R. | |
dc.contributor.author | Pass, Georgia | |
dc.contributor.author | Woods, Julie | |
dc.contributor.author | Lane, David P. | |
dc.contributor.author | Westwood, Nicholas J. | |
dc.date.accessioned | 2012-06-26T14:31:02Z | |
dc.date.available | 2012-06-26T14:31:02Z | |
dc.date.issued | 2008-05-06 | |
dc.identifier.citation | Lain , S , Hollick , J J , Campbell , J , Staples , O D , Higgins , M , Aoubala , M , McCarthy , A , Appleyard , V , Murray , K E , Baker , L , Thompson , A , Mathers , J , Holland , S J , Stark , M J R , Pass , G , Woods , J , Lane , D P & Westwood , N J 2008 , ' Discovery, in vivo activity, and mechanism of action of a small-molecule p53 activator ' , Cancer Cell , vol. 13 , no. 5 , pp. 454-463 . https://doi.org/10.1016/j.ccr.2008.03.004 | en |
dc.identifier.issn | 1535-6108 | |
dc.identifier.other | PURE: 614308 | |
dc.identifier.other | PURE UUID: 22ce04ad-78b2-4bf7-8d20-439473572cfe | |
dc.identifier.other | WOS: 000255569000011 | |
dc.identifier.other | Scopus: 42949114938 | |
dc.identifier.other | ORCID: /0000-0003-0630-0138/work/56424128 | |
dc.identifier.uri | https://hdl.handle.net/10023/2845 | |
dc.description.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. | |
dc.format.extent | 10 | |
dc.language.iso | eng | |
dc.relation.ispartof | Cancer Cell | en |
dc.rights | This is an electronic version of an open access article, published by Cell Press at http://dx.doi.org/10.1016/j.ccr.2008.03.004. Readers are permitted to read, download, print out, extract, reuse, archive, translate and distribute the article provided the appropriate credit is given to the authors and source of the work. | en |
dc.subject | DNA-damage | en |
dc.subject | Immunochemical analysis | en |
dc.subject | Cell-survival | en |
dc.subject | MDM2 | en |
dc.subject | Sirtuins | en |
dc.subject | Deacetylases | en |
dc.subject | Acetylation | en |
dc.subject | Inhibitors | en |
dc.subject | Enzymes | en |
dc.subject | Disease | en |
dc.subject | RC0254 Neoplasms. Tumors. Oncology (including Cancer) | en |
dc.subject | QR180 Immunology | en |
dc.subject | SDG 3 - Good Health and Well-being | en |
dc.subject.lcc | RC0254 | en |
dc.subject.lcc | QR180 | en |
dc.title | Discovery, in vivo activity, and mechanism of action of a small-molecule p53 activator | en |
dc.type | Journal article | en |
dc.description.version | Postprint | en |
dc.contributor.institution | University of St Andrews. School of Chemistry | en |
dc.contributor.institution | University of St Andrews. Biomedical Sciences Research Complex | en |
dc.contributor.institution | University of St Andrews. EaSTCHEM | en |
dc.identifier.doi | https://doi.org/10.1016/j.ccr.2008.03.004 | |
dc.description.status | Peer reviewed | en |
dc.identifier.url | http://www.scopus.com/inward/record.url?scp=42949114938&partnerID=8YFLogxK | en |
dc.identifier.url | http://ukpmc.ac.uk/abstract/MED/18455128 | en |
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