An overview of Sirtuins as potential therapeutic target: Structure, function and modulators

Eur J Med Chem. 2019 Jan 1:161:48-77. doi: 10.1016/j.ejmech.2018.10.028. Epub 2018 Oct 15.


Sirtuin (Yeast Silent Information RegulatorsⅡ, Sir2) was first discovered in the 1970s. Because of its function by removing acetylated groups from histones in the presence of nicotinamide adenine dinucleotide (NAD+), waves of research have assessed the potential of Sirtuin as a therapeutic target. The Sirtuin family, which is widely distributed throughout the nature, has been divided into seven human isoforms (Sirt1-Sirt7). They are thought to be closely related to some aging diseases such as cardiovascular disorders, neurodegeneration, and tumors. Herein, we present a comprehensive review of the structure, function and modulators of Sirtuins, which is expected to be beneficial to relevant studies.

Keywords: Modulators; Protein structures; Sirtuin family; Therapeutic potential.

Publication types

  • Review

MeSH terms

  • Animals
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Molecular Structure
  • Sirtuins / antagonists & inhibitors*
  • Sirtuins / chemistry
  • Sirtuins / metabolism
  • Small Molecule Libraries / chemistry
  • Small Molecule Libraries / pharmacology*
  • Structure-Activity Relationship


  • Enzyme Inhibitors
  • Small Molecule Libraries
  • Sirtuins