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dc.contributor.authorPirrie, Lisa
dc.contributor.authorMcCarthy, Anna R.
dc.contributor.authorMajor, Louise L.
dc.contributor.authorMorkunaite, Vaida
dc.contributor.authorZubriene, Asta
dc.contributor.authorMatulis, Daumantas
dc.contributor.authorLain, Sonia
dc.contributor.authorLebl, Tomas
dc.contributor.authorWestwood, Nicholas J.
dc.date.accessioned2012-12-14T11:31:01Z
dc.date.available2012-12-14T11:31:01Z
dc.date.issued2012-10
dc.identifier.citationPirrie , L , McCarthy , A R , Major , L L , Morkunaite , V , Zubriene , A , Matulis , D , Lain , S , Lebl , T & Westwood , N J 2012 , ' Discovery and validation of SIRT2 inhibitors based on tenovin-6 : use of a 1 H-NMR method to assess deacetylase activity ' , Molecules , vol. 17 , no. 10 , pp. 12206-12224 . https://doi.org/10.3390/molecules171012206en
dc.identifier.issn1420-3049
dc.identifier.otherPURE: 41248378
dc.identifier.otherPURE UUID: dbf38385-1a3e-4372-a990-a6e394a9f2f6
dc.identifier.otherWOS: 000310505400065
dc.identifier.otherScopus: 84868113308
dc.identifier.otherORCID: /0000-0001-5287-4488/work/51010277
dc.identifier.otherORCID: /0000-0002-0269-3221/work/48131725
dc.identifier.otherORCID: /0000-0003-0630-0138/work/56424169
dc.identifier.urihttp://hdl.handle.net/10023/3293
dc.description.abstractThe search for potent and selective sirtuin inhibitors continues as chemical tools of this type are of use in helping to assign the function of this interesting class of deacetylases. Here we describe SAR studies starting from the unselective sirtuin inhibitor tenovin-6. These studies identify a sub-micromolar inhibitor that has increased selectivity for SIRT2 over SIRT1 compared to tenovin-6. In addition, a H-1-NMR-based method is developed and used to validate further this class of sirtuin inhibitors. A thermal shift analysis of SIRT2 in the presence of tenovin-6, -43, a control tenovin and the known SIRT2 inhibitor AGK2 is also presented.
dc.format.extent19
dc.language.isoeng
dc.relation.ispartofMoleculesen
dc.rights© 2012 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).en
dc.subjectSirtuinen
dc.subjectChemical toolen
dc.subjectDeacetylase assayen
dc.subjectNeurodegenerative diseasesen
dc.subjectQD Chemistryen
dc.subjectQH426 Geneticsen
dc.subject.lccQDen
dc.subject.lccQH426en
dc.titleDiscovery and validation of SIRT2 inhibitors based on tenovin-6 : use of a 1H-NMR method to assess deacetylase activityen
dc.typeJournal articleen
dc.contributor.sponsorThe Royal Societyen
dc.contributor.sponsorCancer Research UKen
dc.description.versionPublisher PDFen
dc.contributor.institutionUniversity of St Andrews. School of Chemistryen
dc.contributor.institutionUniversity of St Andrews. School of Biologyen
dc.contributor.institutionUniversity of St Andrews. Biomedical Sciences Research Complexen
dc.contributor.institutionUniversity of St Andrews. EaSTCHEMen
dc.identifier.doihttps://doi.org/10.3390/molecules171012206
dc.description.statusPeer revieweden
dc.identifier.grantnumber516002.K5682/kken
dc.identifier.grantnumberen


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