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Related Experiment Video

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Deacetylation Assays to Unravel the Interplay between Sirtuins SIRT2 and Specific Protein-substrates
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A mini-review on Sirtuin activity assays.

Yan Li1, Ting Liu2, Shanggao Liao2

  • 1School of Basic Medical Science, Guizhou Medical University, Guiyang, Guizhou 550004 China.

Biochemical and Biophysical Research Communications
|October 13, 2015
PubMed
Summary

This review summarizes high-throughput assays for screening sirtuin modulators, crucial for understanding sirtuin biology and developing new therapeutics targeting these NAD-dependent enzymes.

Keywords:
AssaysDeacetylationDeacylationHistone deacetylaseSirtuin

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Enzymology

Background:

  • Sirtuins are NAD-dependent protein lysine deacylases involved in critical cellular processes like transcription, DNA repair, and metabolism.
  • Modulators of sirtuin activity are vital for both fundamental research and the development of novel therapeutic agents.
  • High-throughput assays are essential for efficiently screening small molecules that target sirtuin pathways.

Purpose of the Study:

  • To review and summarize reported high-throughput assays for sirtuin modulators developed between 2000 and 2015.
  • To discuss the performance characteristics of various assays for screening sirtuin modulators.
  • To evaluate the applicability of these assays in high-throughput screening formats for drug discovery and research.

Main Methods:

  • Literature review of published sirtuin assays from 2000-2015.
  • Analysis of assay methodologies, including biochemical and cell-based approaches.
  • Comparative assessment of assay sensitivity, specificity, and suitability for high-throughput screening.

Main Results:

  • A comprehensive overview of diverse assays developed for sirtuin modulation screening.
  • Evaluation of the strengths and limitations of different assay formats in identifying sirtuin modulators.
  • Identification of assays demonstrating high performance for large-scale screening applications.

Conclusions:

  • High-throughput assays are indispensable tools for advancing sirtuin research and therapeutic development.
  • The choice of assay significantly impacts the efficiency and success rate of identifying potent sirtuin modulators.
  • Continued development and optimization of high-throughput assays will accelerate the discovery of sirtuin-targeted drugs and research probes.