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Updated: Jun 27, 2026

Deacetylation Assays to Unravel the Interplay between Sirtuins (SIRT2) and Specific Protein-substrates
Published on: February 27, 2016
Sirtuin modulators: targets for metabolic diseases and beyond
1Sirtris A GSK Company, 200 Technology Square, Cambridge MA 02139, USA. bszczepankiewicz@sirtrispharma.com
Abstract:
Over the past ten years, sirtuins have emerged as an important class of drug targets. These enzymes play an important role in gene activation and silencing in all organisms from prokaryotes to humans. There is evidence that sirtuin modulation can be beneficial for a wide variety of diseases associated with aging. Among these conditions are diabetes, neurodegenerative diseases, and cancer. Agents that activate some sirtuins may be beneficial, while inhibitors of other sirtuins might represent treatment options. This review covers the chemical activators and inhibitors of the sirtuins that have appeared in the literature through the first half of 2008.
Insights
Sirtuins are key drug targets for aging-related diseases like diabetes, neurodegeneration, and cancer. This review details chemical activators and inhibitors of sirtuins published by mid-2008.
Area of Science:
- Biochemistry
- Molecular Biology
- Pharmacology
Background:
- Sirtuins are a class of enzymes crucial for gene regulation across all life forms.
- Emerging evidence links sirtuin activity to aging processes and age-related diseases.
- Modulating sirtuin function presents therapeutic potential for conditions including diabetes, cancer, and neurodegenerative disorders.
Purpose of the Study:
- To review chemical activators and inhibitors of sirtuins.
- To summarize the literature on sirtuin modulators up to the first half of 2008.
Main Methods:
- Literature review of chemical sirtuin modulators.
- Analysis of published data on sirtuin activators and inhibitors.
Main Results:
- Identification of various chemical agents targeting sirtuins.
- Distinction between activating and inhibiting compounds for different sirtuin family members.
Conclusions:
- Sirtuin activators and inhibitors are valuable tools for exploring sirtuin biology.
- Targeting sirtuins offers promising therapeutic strategies for aging-associated diseases.
- Further research into sirtuin modulators is warranted for drug development.
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