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Related Experiment Video

Updated: Mar 26, 2026

Deacetylation Assays to Unravel the Interplay between Sirtuins SIRT2 and Specific Protein-substrates
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A Continuous, Fluorogenic Sirtuin 2 Deacylase Assay: Substrate Screening and Inhibitor Evaluation.

Iacopo Galleano1, Matthias Schiedel2, Manfred Jung2

  • 1Center for Biopharmaceuticals and Department of Drug Design & Pharmacology, University of Copenhagen , Universitetsparken 2, DK-2100, Copenhagen, Denmark.

Journal of Medicinal Chemistry
|January 21, 2016
PubMed
Summary
This summary is machine-generated.

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Researchers developed new assays to study sirtuin 2 (SIRT2) inhibitors, revealing novel enzymatic activities. This work aids in developing pharmaceutical probes for metabolic and transcriptional regulation.

Area of Science:

  • Biochemistry
  • Enzymology
  • Chemical Biology

Background:

  • Sirtuins regulate lysine acylation, crucial for cellular metabolism and transcription.
  • Sirtuin enzymes are key targets for developing pharmaceutical probes.
  • Efficient assays are needed for detailed profiling of sirtuin inhibitors.

Purpose of the Study:

  • To develop readily synthesized fluorogenic substrates for evaluating SIRT2 inhibitors.
  • To enable enzyme-economical, continuous assay formats for SIRT2.
  • To investigate novel enzymatic activities of SIRT2 and profile known inhibitors.

Main Methods:

  • Synthesis of novel fluorogenic substrates for sirtuin evaluation.
  • Development of continuous assay formats for enzyme kinetics.

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  • Profiling of suramin and SirReal2 against modified lysine substrates.

    • Main Results:

    • Established enzyme-economical assays for SIRT2 inhibitor evaluation.
    • Discovered and characterized novel in vitro enzymatic activities of SIRT2.
    • Profiled two known inhibitors, suramin and SirReal2, against various acyllysine substrates.

    Conclusions:

    • Novel fluorogenic substrates facilitate efficient evaluation of SIRT2 inhibitors.
    • SIRT2 exhibits previously unrecognized enzymatic activities warranting further study.
    • The developed assays aid in understanding sirtuin function and inhibitor properties.