Current Trends in Sirtuin Activator and Inhibitor Development. Molecules 2024 Mar 06;29(5)
Date
03/13/2024Pubmed ID
38474697Pubmed Central ID
PMC10934002DOI
10.3390/molecules29051185Scopus ID
2-s2.0-85187801042 (requires institutional sign-in at Scopus site) 12 CitationsAbstract
Sirtuins are NAD+-dependent protein deacylases and key metabolic regulators, coupling the cellular energy state with selective lysine deacylation to regulate many downstream cellular processes. Humans encode seven sirtuin isoforms (Sirt1-7) with diverse subcellular localization and deacylase targets. Sirtuins are considered protective anti-aging proteins since increased sirtuin activity is canonically associated with lifespan extension and decreased activity with developing aging-related diseases. However, sirtuins can also assume detrimental cellular roles where increased activity contributes to pathophysiology. Modulation of sirtuin activity by activators and inhibitors thus holds substantial potential for defining the cellular roles of sirtuins in health and disease and developing therapeutics. Instead of being comprehensive, this review discusses the well-characterized sirtuin activators and inhibitors available to date, particularly those with demonstrated selectivity, potency, and cellular activity. This review also provides recommendations regarding the best-in-class sirtuin activators and inhibitors for practical research as sirtuin modulator discovery and refinement evolve.
Author List
Bursch KL, Goetz CJ, Smith BCAuthor
Brian C. Smith PhD Associate Professor in the Biochemistry department at Medical College of WisconsinMESH terms used to index this publication - Major topics in bold
HumansLysine
Protein Isoforms
Sirtuin 1
Sirtuins
