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KID-1/kinaseinducedbydepolarization|kinaseinducedbydepolarization|pim-3oncogene|Pim-3proto-oncogene
Description:Crystalstructureofhumanproto-oncogeneserinethreoninekinase(PIM1)incomplexwithaconsensuspeptideandabetacarbolineligandII.
Downloadallstructure-activitydataforthistargetasaCSVfile
EMDMilliporeKinaseProfilerTMscreen/ReactionBiologyKinaseHotspotSMscreen
Ascreenprofiling158kinaseinhibitors(CalbiochemProteinKinaseInhibitorLibraryIandII,cataloguenumbers539744and539745)fortheirinhibitoryactivityat1Mand10Magainst234humanrecombinantkinasesusingtheEMDMilliporeKinaseProfilerTMservice.
Ascreenprofilingtheinhibitoryactivityof178commerciallyavailablekinaseinhibitorsat0.5Magainstapanelof300recombinantproteinkinasesusingtheReactionBiologyCorporationKinaseHotspotSMplatform.
http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx
1.AnastassiadisT,DeaconSW,DevarajanK,MaH,PetersonJR.(2011)Comprehensiveassayofkinasecatalyticactivityrevealsfeaturesofkinaseinhibitorselectivity.
2.BurgerMT,HanW,LanJ,NishiguchiG,BellamacinaC,LindvalM,AtallahG,DingY,MathurM,McBrideCetal..(2013)StructureGuidedOptimization,inVitroActivity,andinVivoActivityofPan-PIMKinaseInhibitors.
3.BurgerMT,NishiguchiG,HanW,LanJ,SimmonsR,AtallahG,DingY,TamezV,ZhangY,MathurMetal..(2015)IdentificationofN-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide(PIM447),aPotentandSelectiveProviralInsertionSiteofMoloneyMurineLeukemia(PIM)1,2,and3KinaseInhibitorinClinicalTrialsforHematologicalMalignancies.
4.DavisMI,HuntJP,HerrgardS,CiceriP,WodickaLM,PallaresG,HockerM,TreiberDK,ZarrinkarPP.(2011)Comprehensiveanalysisofkinaseinhibitorselectivity.
5.DowlingJE,AlimzhanovM,BaoL,BlockMH,ChuaquiC,CookeEL,DenzCR,HirdA,HuangS,LarsenNAetal..(2013)StructureandPropertyBasedDesignofPyrazolo[1,5-a]pyrimidineInhibitorsofCK2KinasewithActivityinVivo.
6.DryginD,HaddachM,PierreF,RyckmanDM.(2012)PotentialuseofselectiveandnonselectivePimkinaseinhibitorsforcancertherapy.
7.GaoY,DaviesSP,AugustinM,WoodwardA,PatelUA,KovelmanR,HarveyKJ.(2013)Abroadactivityscreeninsupportofachemogenomicmapforkinasesignallingresearchanddrugdiscovery.
8.GarciaPD,LangowskiJL,WangY,ChenM,CastilloJ,FantonC,IsonM,ZavorotinskayaT,DaiY,LuJetal..(2014)Pan-PIMkinaseinhibitionprovidesanoveltherapyfortreatinghematologiccancers.
9.HaddachM,MichauxJ,SchwaebeMK,PierreF,O"BrienSE,BorsanC,TranJ,RaffaeleN,RavulaS,DryginDetal..(2012)DiscoveryofCX-6258.APotent,Selective,andOrallyEfficaciouspan-PimKinasesInhibitor.
10.HuberK,BraultL,FedorovO,GasserC,FilippakopoulosP,BullockAN,FabbroD,TrappeJ,SchwallerJ,KnappSetal..(2012)7,8-dichloro-1-oxo-β-carbolinesasaversatilescaffoldforthedevelopmentofpotentandselectivekinaseinhibitorswithunusualbindingmodes.
11.KoblishH,LiYL,ShinN,HallL,WangQ,WangK,CovingtonM,MarandoC,BowmanK,BoerJetal..(2018)PreclinicalcharacterizationofINCB053914,anovelpan-PIMkinaseinhibitor,aloneandincombinationwithanticanceragents,inmodelsofhematologicmalignancies.
12.PierreF,StefanE,NédellecAS,ChevrelMC,ReganCF,Siddiqui-JainA,MacalinoD,StreinerN,DryginD,HaddachMetal..(2011)7-(4H-1,2,4-Triazol-3-yl)benzo[c][2,6]naphthyridines:anovelclassofPimkinaseinhibitorswithpotentcellantiproliferativeactivity.
13.WodickaLM,CiceriP,DavisMI,HuntJP,FloydM,SalernoS,HuaXH,FordJM,ArmstrongRC,ZarrinkarPPetal..(2010)Activationstate-dependentbindingofsmallmoleculekinaseinhibitors:structuralinsightsfrombiochemistry.
PIMfamily:Pim-3proto-oncogene,serine/threoninekinase.Lastmodifiedon23/01/2020.Accessedon18/05/2020.IUPHAR/BPSGuidetoPHARMACOLOGY,http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2160.
