title: A patent review of sirtuin activators: an update.
abstract: BACKGROUND
  Reversible acetylation is a key post-translational modification of target proteins. Sirtuin deacetylases represent the homolog of the yeast silent information regulator (SIR2). Although seven sirtuins have been found in mammals, all sirtuin activators described to date act through SIRT1.
  
  
  METHODS
  Areas covered in this paper include a review of the patent literature associated with SIRT1 activators, with a focus on therapeutic applications, primarily related to the use of pharmaceuticals and nutraceuticals containing resveratrol (RSV), and the development of second-generation activators unrelated to RSV. Also discussed is the current controversy over whether or not these molecules are actual SIRT1 activators.
  
  
  CONCLUSIONS
  Developing effective strategies to protect against diet-induced metabolic imbalance is necessary to fight against current obesity rates. The hypothalamus is a candidate for developing drugs that suppress SIRT1 degradation, as a strategy for treating metabolic syndrome. Deciphering the basic mechanism of activators is essential to develop effective strategies to alter sirtuin activity. This is true regardless of the apparent controversy of whether in vitro activation of SIRT1 is direct or not, depending on the experimental design, and whether sirtuins may play a major role in longevity. The numerous studies on their positive effects against age-related diseases, obesity and other metabolic disorders are still valid, promising to positively influence the development of treatments to improve human health.
authors.affiliation: Departamento de Biología Celular, Fisiología e Inmunología, Facultad de Ciencias, Campus Universitario de Rabanales, Universidad de Córdoba, Spain.
authors.forename: José M
authors.initials: JM
authors.lastname: Villalba
authors.forename: Rafael
authors.initials: R
authors.lastname: de Cabo
authors.forename: Francisco J
authors.initials: FJ
authors.lastname: Alcain
mesh_terms: D000818:Animals; D019440:Anti-Obesity Agents / Q000494:pharmacology; D019587:Dietary Supplements; D015195:Drug Design; D004789:Enzyme Activation; D020536:Enzyme Activators / Q000737:chemistry / Q000494:pharmacology*; D006576:Heterocyclic Compounds, 4 or More Rings / Q000494:pharmacology; D006801:Humans; D015394:Molecular Structure; D010330:Patents as Topic; D000077185:Resveratrol; D056564:Sirtuin 1 / Q000378:metabolism*; D013267:Stilbenes / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D019440:Anti-Obesity Agents; D020536:Enzyme Activators; D006576:Heterocyclic Compounds, 4 or More Rings; C525422:SRT1720; D013267:Stilbenes; D056564:Sirtuin 1; D000077185:Resveratrol