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Issue 7, 2011
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N1-Benzyl substituted cambinol analogues as isozyme selective inhibitors of the sirtuin family of protein deacetylases

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Abstract

The human deacetylase SIRT2 is believed to promote neurodegeneration with recent studies demonstrating that a reduction in the activity of SIRT2 can rescue alpha synuclein toxicity in Parkinson's disease models. In contrast, a second member of the sirtuin family, SIRT1, is believed to play a neuroprotective role. This dichotomy places an additional challenge in the path of sirtuin inhibitor development as a need for isozyme selectivity arises. By combining computational methods with assessment of the biological activity of novel N1-substituted cambinol analogues, further insights that are relevant to this challenge are obtained.

Graphical abstract: N1-Benzyl substituted cambinol analogues as isozyme selective inhibitors of the sirtuin family of protein deacetylases

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Publication details

The article was received on 21 Jan 2011, accepted on 21 Mar 2011 and first published on 05 May 2011


Article type: Concise Article
DOI: 10.1039/C1MD00023C
Med. Chem. Commun., 2011,2, 611-615

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    N1-Benzyl substituted cambinol analogues as isozyme selective inhibitors of the sirtuin family of protein deacetylases

    F. Medda, T. L. Joseph, L. Pirrie, M. Higgins, A. M. Z. Slawin, S. Lain, C. Verma and N. J. Westwood, Med. Chem. Commun., 2011, 2, 611
    DOI: 10.1039/C1MD00023C

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