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Your search keyword '"deacetylase assay"' showing total 3 results
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3 results on '"deacetylase assay"'

1. Discovery and Validation of SIRT2 Inhibitors Based on Tenovin-6: Use of a 1H-NMR Method to Assess Deacetylase Activity

Author

Nicholas J. Westwood, Sonia Lain, Tomas Lebl, Daumantas Matulis, Asta Zubrienė, Anna R. McCarthy, Louise L. Major, Vaida Morkūnaitė, and Lisa Pirrie

Subjects
sirtuin, chemical tool, deacetylase assay, neurodegenerative diseases, Organic chemistry, QD241-441
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 1H-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.

Published
2012
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2. Discovery and Validation of SIRT2 Inhibitors Based on Tenovin-6: Use of a 1H-NMR Method to Assess Deacetylase Activity.

Author

Pirrie, Lisa, McCarthy, Anna R., Major, Louise L., Morkūnaitė, Vaida, Zubrienė, Asta, Matulis, Daumantas, Lain, Sonia, Lebl, Tomas, and Westwood, Nicholas J.

Subjects
*ENZYME inhibitors synthesis, *NUCLEAR magnetic resonance, *DEACETYLASES, *SIRTUINS, *THERMAL analysis
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 1H-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. [ABSTRACT FROM AUTHOR]

Published
2012
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3. Discovery and Validation of SIRT2 Inhibitors Based on Tenovin-6: Use of a 1H-NMR Method to Assess Deacetylase Activity

Author

Anna R. McCarthy, Sonia Lain, Nicholas J. Westwood, Vaida Morkūnaitė, Asta Zubrienė, Daumantas Matulis, Lisa Pirrie, Tomas Lebl, Louise L. Major, The Royal Society, Cancer Research UK, University of St Andrews. School of Chemistry, University of St Andrews. School of Biology, University of St Andrews. Biomedical Sciences Research Complex, and University of St Andrews. EaSTCHEM

Subjects
Chemical tool, chemical tool, Pharmaceutical Science, deacetylase assay, QH426 Genetics, Computational biology, Biology, SIRT2, Article, Analytical Chemistry, Histones, lcsh:QD241-441, Sirtuin 2, lcsh:Organic chemistry, sirtuin, neurodegenerative diseases, Drug Discovery, Sirtuin, Humans, QD, Physical and Theoretical Chemistry, Enzyme Inhibitors, QH426, Nuclear Magnetic Resonance, Biomolecular, Deacetylase assay, Neurodegenerative diseases, Organic Chemistry, Reproducibility of Results, Acetylation, QD Chemistry, Enzyme Activation, Biochemistry, Chemistry (miscellaneous), Benzamides, Proton NMR, biology.protein, Molecular Medicine, Deacetylase activity
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. Publisher PDF

Published
2012
Full Text
View/download PDF

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