title: Sirtuin catalysis and regulation.
abstract: Sirtuins are a family of NAD(+)-dependent protein deacetylases/deacylases that dynamically regulate transcription, metabolism, and cellular stress response. Their general positive link with improved health span in mammals, potential regulation of pathways mediated by caloric restriction, and growing links to human disease have spurred interest in therapeutics that target their functions. Here, we review the current understanding of the chemistry of catalysis, biological targets, and endogenous regulation of sirtuin activity. We discuss recent efforts to generate small-molecule regulators of sirtuin activity.
authors.affiliation: Department of Biomolecular Chemistry and the Wisconsin Institute for Discovery, University of Wisconsin, Madison, Wisconsin 53715, USA. jmdenu@wisc.edu
authors.forename: Jessica L
authors.initials: JL
authors.lastname: Feldman
authors.forename: Kristin E
authors.initials: KE
authors.lastname: Dittenhafer-Reed
authors.forename: John M
authors.initials: JM
authors.lastname: Denu
mesh_terms: D000215:Acylation / Q000187:drug effects; D000818:Animals; D055162:Biocatalysis / Q000187:drug effects; D006801:Humans; D037761:Sirtuins / Q000737:chemistry / Q000378:metabolism*; D054852:Small Molecule Libraries / Q000494:pharmacology; D013379:Substrate Specificity / Q000187:drug effects
chemical_list: D054852:Small Molecule Libraries; D037761:Sirtuins