Description
BrefeldinAisalactoneantibioticfoundinfungisuchasEupenicillium;itexhibitsanticancerandantiviralactivities.BrefeldinAinhibitsactivityofguaninenucleotideexchangefactors,preventingassociationwithCOPIandCOPI-mediatedvesicleformationandsuppressingproteintransportfromtheendoplasmicreticulumtotheGolgiapparatus.BrefeldinAisusedinresearchmodelstostudyendoplasmicreticulumstressandproteintransport.Invitro,thiscompoundinhibitspoliovirusreplication.Inprostatecancercells,brefeldinAinhibitscellgrowth,inducesapoptosisandG1phasecellcyclearrest,decreaseslevelsofp53,CDK2,CDK4,andcyclinD1,andcausescelldeath.
References
ZhouC,LiC,LiD,etal.BIG1,abrefeldinA-inhibitedguaninenucleotide-exchangeproteinregulatesneuritedevelopmentviaPI3K-AKTandERKsignalingpathways.Neuroscience.2013Dec19;254:361-8.PMID:24090963.
RouhanaJ,PADIllaA,EstaranS,etal.KineticsofinteractionbetweenADP-ribosylationfactor-1(Arf1)andtheSec7domainofArnoguaninenucleotideexchangefactor,modulationbyallostericfactors,andtheuncompetitiveinhibitorbrefeldinA.JBiolChem.2013Feb15;288(7):4659-72.PMID:23255605.
ChapmanJR,TazakiH,MallouhC,etal.BrefeldinA-inducedapoptosisinprostaticcancerDU-145cells:apossIBLep53-independentdeathpathway.BJUInt.1999Apr;83(6):703-8.PMID:10233583.
CuconatiA,MollaA,WimmerE.BrefeldinAinhibitscell-free,denovosynthesisofpoliovirus.JVirol.1998Aug;72(8):6456-64.PMID:9658088.