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dc.contributor.authorSinclair, David Andrew
dc.contributor.authorGuarente, Leonard
dc.date.accessioned2018-02-23T21:05:49Z
dc.date.issued2014
dc.identifierQuick submit: 2014-01-09T09:17:26-05:00
dc.identifier.citationSinclair, David A., and Leonard Guarente. 2014. “Small-Molecule Allosteric Activators of Sirtuins.” Annual Review of Pharmacology and Toxicology 54 (1) (January 6): 363–380. doi:10.1146/annurev-pharmtox-010611-134657.en_US
dc.identifier.issn0362-1642en_US
dc.identifier.urihttp://nrs.harvard.edu/urn-3:HUL.InstRepos:34865300
dc.description.abstractThe mammalian sirtuins (SIRT1-7) are NAD(+)-dependent lysine deacylases that play central roles in cell survival, inflammation, energy metabolism, and aging. Members of this family of enzymes are considered promising pharmaceutical targets for the treatment of age-related diseases including cancer, type 2 diabetes, inflammatory disorders, and Alzheimer's disease. SIRT1-activating compounds (STACs), which have been identified from a variety of chemical classes, provide health benefits in animal disease models. Recent data point to a common mechanism of allosteric activation by natural and synthetic STACs that involves the binding of STACs to a conserved N-terminal domain in SIRT1. Compared with polyphenols such as resveratrol, the synthetic STACs show greater potency, solubility, and target selectivity. Although considerable progress has been made regarding SIRT1 allosteric activation, key questions remain, including how the molecular contacts facilitate SIRT1 activation, whether other sirtuin family members will be amenable to activation, and whether STACs will ultimately prove safe and efficacious in humans.en_US
dc.language.isoen_USen_US
dc.publisherAnnual Reviewsen_US
dc.relation.isversionofdoi:10.1146/annurev-pharmtox-010611-134657en_US
dash.licenseMETA_ONLY
dc.subjectaging, sirtuin, NAD, allosteric activation, HDACen_US
dc.titleSmall-Molecule Allosteric Activators of Sirtuinsen_US
dc.typeJournal Articleen_US
dc.date.updated2014-01-09T14:18:45Z
dc.description.versionVersion of Recorden_US
dc.rights.holderGuarente and Sinclair
dc.relation.journalAnnual Review of Pharmacology and Toxicologyen_US
dash.depositing.authorSinclair, David Andrew
dash.embargo.until10000-01-01
dc.identifier.doi10.1146/annurev-pharmtox-010611-134657*
workflow.legacycommentsnoap.noneen_US
dash.contributor.affiliatedSinclair, David


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