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

Federico Medda, Thomas L. Joseph, Lisa Pirrie, Maureen Higgins, Alexandra M. Z. Slawin, Sonia Lain, Chandra Verma, Nicholas J. Westwood

Research output: Contribution to journalArticlepeer-review

12 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)611-615
Number of pages5
JournalMedChemComm
Volume2
Issue number7
DOIs
Publication statusPublished - Jul 2011

Keywords

  • ENZYMES

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