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Updated: May 4, 2026
Deacetylation Assays to Unravel the Interplay between Sirtuins SIRT2 and Specific Protein-substrates
Published on: February 27, 2016
New assays and approaches for discovery and design of Sirtuin modulators
Mike Schutkowski1, Frank Fischer, Claudia Roessler
1Martin Luther University Halle-Wittenberg, Institute for Biochemistry and Biotechnology, Department of Enzymology , 06108 Halle , Germany.
Introduction:
Sirtuins are an evolutionarily conserved family of NAD(+)-dependent protein lysine deacylases. In mammals, 7 Sirtuin isoforms control various functions in metabolism, stress responses and aging processes. Sirtuins are considered attractive therapeutic targets for metabolic and aging-related diseases, such as metabolic syndrome and neurodegenerative disorders. Extensive development efforts on small-molecule Sirtuin inhibitors and activators have yielded few potent and selective compounds, partly due to shortcomings of available assays and a lack of mechanistic characterization of identified compounds.
Areas Covered:
The authors describe the developments in analyzing Sirtuin activity and conceptual advances in the identification, improvement and design of Sirtuin-modulating compounds. They also review the application of these methods and concepts for the development and mechanistic characterization of Sirtuin modulators.
Expert Opinion:
Novel assays and experimental approaches for studying Sirtuin activity have been instrumental for major progress in understanding functions of Sirtuins and how these enzymes can be modulated with drugs. The improved tools and mechanistic insights now enable a more efficient development of Sirtuin modulators for in vivo studies and therapeutic applications.
Insights
Novel assays and experimental approaches enhance the development of Sirtuin modulators. Improved tools and mechanistic insights accelerate drug development for metabolic and aging-related diseases.
Area of Science:
- Biochemistry
- Molecular Biology
- Pharmacology
Background:
- Sirtuins are NAD(+)-dependent protein lysine deacylases with crucial roles in metabolism, stress, and aging.
- Mammalian Sirtuins (7 isoforms) are therapeutic targets for metabolic and neurodegenerative diseases.
- Developing selective Sirtuin modulators is challenging due to assay limitations and poor mechanistic understanding.
Purpose of the Study:
- To review advancements in analyzing Sirtuin activity.
- To discuss conceptual progress in identifying and designing Sirtuin modulators.
- To highlight the application of these methods for Sirtuin modulator development and characterization.
Main Methods:
- Review of novel assays for Sirtuin activity analysis.
- Examination of conceptual advances in Sirtuin modulator design.
- Analysis of methods for mechanistic characterization of Sirtuin modulators.
Main Results:
- Significant progress in understanding Sirtuin functions and modulation.
- Development of novel assays and experimental approaches.
- Identification of improved tools and mechanistic insights.
Conclusions:
- Novel assays and approaches are key to understanding Sirtuin functions and drug modulation.
- Improved tools and insights facilitate efficient Sirtuin modulator development.
- Enhanced development enables in vivo studies and therapeutic applications for Sirtuin-related diseases.
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