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Discovery and validation of SIRT2 inhibitors based on tenovin-6 : use of a 1H-NMR method to assess deacetylase activity

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Pirrie2012molecules_17_12206_v2.pdf (504.7Kb)
Date
10/2012
Author
Pirrie, Lisa
McCarthy, Anna R.
Major, Louise L.
Morkunaite, Vaida
Zubriene, Asta
Matulis, Daumantas
Lain, Sonia
Lebl, Tomas
Westwood, Nicholas J.
Funder
The Royal Society
Cancer Research UK
Grant ID
516002.K5682/kk
Keywords
Sirtuin
Chemical tool
Deacetylase assay
Neurodegenerative diseases
QD Chemistry
QH426 Genetics
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Abstract
The 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.
Citation
Pirrie , 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/molecules171012206
Publication
Molecules
Status
Peer reviewed
DOI
https://doi.org/10.3390/molecules171012206
ISSN
1420-3049
Type
Journal article
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/).
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  • University of St Andrews Research
URI
http://hdl.handle.net/10023/3293

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