Description
PAC-1(ProcaspaseActivatingCompound1)hasbeenidentifiedthroughhigh-throughputscreeningasacompoundthatmayenhancetheenzymaticactivityofprocaspase-3invitro.Procaspase-3maybeusefulasananticancerstrategyduetoitslowfrequencyofmutationsincancerandexpressionofitsenzymeinseveraltypesofcancers.PAC-1convertsprocaspase-3toactivecaspase-3invitrobychelatingzincionsandtherebyinducingcelldeathinthetumorcells.Inmultiplecancercelllines,PAC-1wasshowntotriggerendoplasmicreticulumstresssignalingandinduceautophagyandmitochondria-mediatedapotosis.
References
SarkarA,BalakrishnanK,ChenJ,etal.MolecularevidenceofZnchelationoftheprocaspaseactivatingcompoundB-PAC-1inBcelllymphoma.Oncotarget.2016Jan19;7(3):3461-3476.PMID:26658105.
RothHS,HergenrotherPJ.Derivativesofprocaspase-activatingcompound1(PAC-1)andtheiranticanceractivities.CurrMedChem.2016;23(3):201-241.PMID:26630918.
SeerviM,SobhanPK,JosephJ,etal.ERO1alpha-dependentendoplasmicreticulum-mitochondrialcalciumfluxcontributestoERstressandmitochondrialpermeABIlizationbyprocaspase-activatingcompound-1(PAC-1).CellDeathDis.2013Dec19;4:e968.PMID:24357799.
LucasPW,SchmitJM,PetersonQP,etal.PharmacokineticsandderivationofananticancerdosingregimenforPAC-1,apreferentialsmallmoleculeactivatorofprocaspase-3,inhealthydogs.InvestNewDrugs.2011Oct;29(5):901-911.PMID:20499133.
PetersonQP,GoodeDR,WestDC,etal.PAC-1activatesprocaspase-3invitrothroughreliefofzinc-mediatedinhibition.JMolBiol.2009Apr24;388(1):144-158.PMID:19281821.
美国LKT Labs 是一家专注于防癌抗癌特殊化学品研究和开发的公司。主要提供：癌症药物、药物发现试剂盒、天然产物、广泛的生命科学研究试剂、定制合成。
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