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Updated: Jun 29, 2026

Deacetylation Assays to Unravel the Interplay between Sirtuins (SIRT2) and Specific Protein-substrates
Published on: February 27, 2016
Sirtuins--novel therapeutic targets to treat age-associated diseases
Siva Lavu1, Olivier Boss, Peter J Elliott
1Sirtris Pharmaceuticals, Cambridge, Massachusetts 02139, USA.
Abstract:
Sirtuins post-translationally modulate the function of many cellular proteins that undergo reversible acetylation-deacetylation cycles, affecting physiological responses that have implications for treating diseases of ageing. Potent small-molecule modulators of sirtuins have shown efficacy in preclinical models of metabolic, neurodegenerative and inflammatory diseases, and so hold promise for drug discovery efforts in multiple therapeutic areas. Here, we discuss current knowledge and data that strengthens sirtuins as a druggable set of enzymes for the treatment of age-associated diseases, including activation of SIRT1 in type 2 diabetes.
Insights
Sirtuins are enzymes crucial for aging diseases. Small molecules targeting sirtuins show promise for treating metabolic, neurodegenerative, and inflammatory conditions, offering new therapeutic avenues.
Area of Science:
- Biochemistry
- Molecular Biology
- Gerontology
Background:
- Sirtuins regulate protein acetylation, impacting cellular processes relevant to aging.
- Dysregulation of sirtuin activity is linked to age-associated diseases.
- Small-molecule sirtuin modulators are emerging as potential therapeutics.
Purpose of the Study:
- To review current knowledge on sirtuins as druggable targets.
- To highlight the therapeutic potential of sirtuin modulation in age-related diseases.
- To discuss the activation of SIRT1 for type 2 diabetes treatment.
Main Methods:
- Literature review of sirtuin research.
- Analysis of preclinical data for sirtuin modulators.
- Discussion of sirtuin's role in disease pathophysiology.
Main Results:
- Sirtuins are validated druggable targets.
- Small-molecule modulators demonstrate efficacy in preclinical models.
- Sirtuin activation shows promise for treating metabolic diseases like type 2 diabetes.
Conclusions:
- Sirtuins represent a promising class of enzymes for drug discovery.
- Targeting sirtuins offers therapeutic potential for multiple age-associated diseases.
- Further research into sirtuin modulators could lead to novel treatments.
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