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Updated: Mar 19, 2026

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Small Molecules as SIRT Modulators.

Xinfa Bai1, Lei Yao1, Xuan Ma1

  • 1School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation, Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, Yantai 264005, China.

Mini Reviews in Medicinal Chemistry
|June 24, 2016
PubMed
Summary
This summary is machine-generated.

Small molecules modulating sirtuins (NAD+-dependent deacetylases) show potential for treating diseases like cancer and aging. This review covers natural and synthetic compounds affecting sirtuin activity.

Keywords:
Class III histone deacetylasesSirtuinSuRTVirus infectionmodulatorssmall molecules.

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Sirtuins are NAD+-dependent deacetylases with diverse cellular locations and functions.
  • They play critical roles in biological processes including aging, longevity, and metabolic homeostasis.
  • Dysregulation of sirtuin activity is implicated in various human diseases.

Purpose of the Study:

  • To review small molecules that modulate sirtuin activity.
  • To understand the interaction between small molecules and sirtuins.
  • To highlight the therapeutic potential of sirtuin modulators.

Main Methods:

  • High-throughput screening (HTS) and medicinal chemistry techniques were employed.
  • Identification of compounds with SIRT inhibitory or activation effects.
  • Review of existing literature on natural and synthetic sirtuin modulators.

Main Results:

  • Polyphenolic compounds like Resveratrol, Fisetin, and Quercetin activate SIRT1.
  • Synthetic compounds such as SRT1720 and Selisistat modulate sirtuin activity.
  • These modulators show therapeutic potential for diseases including cancer, neurodegeneration, and aging.

Conclusions:

  • Small molecule modulators offer promising therapeutic strategies for sirtuin-related diseases.
  • Further research into small molecule-sirtuin interactions can advance drug development.
  • Targeting sirtuins holds potential for treating age-related and other chronic conditions.