Description
ABT-737isaBH3mimeticthatactsasaninhibitorofBcl-2,Bxl-xl,andBcl-ω.ABT-737exhibitsanticancerchemotherapeuticandantithromboticactivities.ABT-737iscurrentlyinclinicaltrialsasonecomponentofacombinationtherapyinthetreatmentofvariouscancerssuchasacutemyelogenousleukemia(AML).ThiscompoundinhibitsgrowthofAMLcellsinvitroandincreasessurvivalratesandLifespaninanimalmodelsofAML.Invitro,ABT-737inducesmitochondrialmembranedepolarizationinplatelets,inducingapoptosisandclearance.
References
LieberJ,Armeanu-EbingerS,FuchsJ.TheRoleofBH3-MimeticDrugsintheTreatmentofPediatricHepatoblastoma.IntJMolSci.2015Feb16;16(2):4190-4208.PMID:25690034.
BaevDV,KrawczykJ,O’DwyerM,etal.TheBH3-mimeticABT-737effectivelykillsacutemyeloidleukemiainitiatingcells.LeukResRep.2014Sep1;3(2):79-82.PMID:25379408.
GyulkhandanyanAV,MutluA,AllenDJ,etal.BH3-mimeticABT-737inducesstrongmitochondrialmembranedepolarizationinplateletsbutonlyweaklystimulatesapoptoticmorphologicalchanges,plateletshrinkageandmicroparticleformation.ThrombRes.2014Jan;133(1):73-9.PMID:24268298.
BeurletS,OmidvarN,GorombeiP,etal.BCL-2inhibitionwithABT-737prolongssurvivalinanNRAS/BCL-2mousemodelofAMLbytargetingprimitiveLSKandProgenitorcells.Blood.2013Oct17;122(16):2864-76.PMID:23943652.