Related Experiment Video

Updated: Jun 14, 2025

Deacetylation Assays to Unravel the Interplay between Sirtuins SIRT2 and Specific Protein-substrates
14:32

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

Published on: February 27, 2016

8.3K

Activation and inhibition of sirtuins: From bench to bedside

Francesco Fiorentino1, Emanuele Fabbrizi1, Antonello Mai1,2

  • 1Department of Drug Chemistry and Technologies, Sapienza University of Rome, Rome, Italy.

Medicinal Research Reviews
|August 31, 2024
PubMed

Insights

Sirtuins, NAD+-dependent enzymes, regulate key cellular processes and aging. Modulating sirtuins offers therapeutic potential for metabolic, cardiovascular, and neurodegenerative diseases, and cancer.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Sirtuins are NAD+-dependent enzymes regulating genomic stability, gene expression, metabolism, and aging.
  • Dysregulation of sirtuins is implicated in metabolic, cardiovascular, neurological diseases, and cancer.
  • Sirtuins exhibit context-dependent roles in cancer, acting as tumor suppressors or promoters.

Purpose of the Study:

  • To provide critical insights into sirtuin pharmacology, enzymatic activities, and biological functions.
  • To review relevant sirtuin modulators, including their mechanisms, structure-activity relationships, and effects.
  • To discuss the therapeutic potential of sirtuin modulation in age-related diseases and cancer.

Main Methods:

  • Literature review of sirtuin biology and pharmacology.
  • Analysis of enzymatic activities and biological functions of sirtuins.
  • Overview of structure-activity relationships and pharmacological effects of sirtuin modulators.

Main Results:

  • Sirtuins are crucial for cellular homeostasis and organism wellness.
  • Sirtuin modulation shows therapeutic promise for diabetes, cardiovascular/neurodegenerative disorders, and cancer.
  • Isoform-selective modulators can advance understanding of sirtuin biology and therapeutic development.

Conclusions:

  • Sirtuin modulators represent a promising therapeutic strategy for various diseases.
  • Further research into isoform-selective sirtuin modulators is warranted.
  • Understanding sirtuin pharmacology is key to developing effective treatments for age-related conditions and cancer.
Keywords:
cancerdrug discoverymetabolismprotein lysine deacylationsirtuins

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