Description
SRT1720isaninhibitorofsirtuin3(SIRT3)andactivatorofsirtuin1(SIRT1);sirtuinsareconsideredclassIIIhistonedeacetylases(HDACs).SRT1720exhibitsnephroprotective,anti-aging,anti-inflammatory,andpro-angiogenicactivities.SRT1720bindstheacetyl-LyssiteonsirtuinsratherthantheNAD+site.Inanimalmodelsofkidneyischemia/reperfusioninjury,SRT1720improvesrenaltubularpathologyandoverallrenalfunction.Inanimalmodelsfedhighfatdiets,SRT1720delaystheonsetofmetabolicdiseasesanddecreaseslevelsofpro-inflammatorycytokines,extendinganimalLifespan.Inanimalmodelsofmaculardegeneration,thiscompoundsuppressesactivationofNF-κBandreleaseofIL-6,IL-8,andMMP-9,decreasingamyloid-β(Aβ)-inducedretinalpigmentepithelialbarrierdisruption.Additionally,SRT1720increasesVEGFsecretionandpromotesmigrationandmetastasisofbreastcancercellsinvitroandinvivo.
References
MitchellSJ,Martin-MontalvoA,MerckenEM,etal.TheSIRT1ActivatorSRT1720ExtendsLifespanandImprovesHealthofMiceFedaStandardDiet.CellRep.2014Mar13;6(5):836-43.PMID:24582957.
CaoL,LiuC,WangF,etal.SIRT1negativelyregulatesamyloid-beta-inducedinflammationviatheNF-κBpathway.BrazJMedBiolRes.2013Aug;46(8):659-69.PMID:24036938.
NguyenGT,SchaeferS,GertzM,etal.Structuresofhumansirtuin3complexeswithADP-riboseandwithcarba-NAD+andSRT1720:bindingdetailsandinhibitionmechanism.ActaCrystallogrDBiolCrystallogr.2013Aug;69(Pt8):1423-32.PMID:23897466.
FanH,YangHC,YouL,etal.Thehistonedeacetylase,SIRT1,contributestotheresistanceofyoungmicetoischemia/reperfusion-inducedacutekidneyinjury.KidneyInt.2013Mar;83(3):404-13.PMID:23302720.
SuzukiK,HayashiR,IchikawaT,etal.SRT1720,aSIRT1activator,promotestumorcellmigration,andlungmetastasisofbreastcancerinmice.OncolRep.2012Jun;27(6):1726-32.PMID:22470132.
