Related Experiment Video

Updated: Sep 16, 2025

Deacetylation Assays to Unravel the Interplay between Sirtuins SIRT2 and Specific Protein-substrates
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Deacetylation Assays to Unravel the Interplay between Sirtuins SIRT2 and Specific Protein-substrates

Published on: February 27, 2016

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Sirtuin 3 as a promising target in disease therapy: Model action and drug discovery

Dongmin Yu1

  • 1Department of Breast Disease Comprehensive Center, First Affiliated Hospital of Gannan Medical University, Ganzhou, 341000, China.

European Journal of Medicinal Chemistry
|July 10, 2025
PubMed

Insights

Sirtuin 3 (SIRT3) is a key enzyme in epigenetic regulation linked to various diseases. This review explores SIRT3 modulators as promising therapeutic targets for conditions like cancer and cardiovascular disease.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Sirtuin 3 (SIRT3) is a Class III histone deacetylase (HDACIII) crucial for epigenetic regulation.
  • Aberrant SIRT3 expression is implicated in inflammation, cancer, cardiovascular diseases, and central nervous system disorders.
  • SIRT3 regulates vital intracellular processes including cell migration and apoptosis, positioning it as a therapeutic target.

Purpose of the Study:

  • To review the structure and pharmacological actions of SIRT3.
  • To analyze cocrystal structures of SIRT3 inhibitors and activators.
  • To discuss the drug design and development of SIRT3 modulators.

Main Methods:

  • Literature review of SIRT3 structure, function, and modulators.
  • Analysis of cocrystal structures of SIRT3 inhibitors/activators.
  • Examination of recent drug design strategies for SIRT3 modulators.

Main Results:

  • SIRT3's structure and pharmacological roles are summarized.
  • Cocrystal structures reveal insights into inhibitor/activator binding.
  • Recent advancements in designing small-molecule SIRT3 modulators are highlighted.

Conclusions:

  • SIRT3 modulators represent a promising therapeutic avenue for various diseases.
  • Understanding SIRT3 structure-activity relationships is key for drug development.
  • Challenges in small-molecule modulator discovery and future directions are presented.
Keywords:
ActivatorsChallengesInhibitorsModulatorsSirtuin 3

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