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PKCM|PRKCM|serine/threonine-proteinkinaseD1|PKC-mu
Downloadallstructure-activitydataforthistargetasaCSVfile

Description:Measuringinhibitionofsyntheticsubstratephosphorylationinatime-resolvedfluorescenceresonanceenergytransfer(TR-FRET)assay.
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.Bravo-AltamiranoK,GeorgeKM,FrantzMC,LavalleCR,TandonM,LeimgruberS,SharlowER,LazoJS,WangQJ,WipfP.(2011)SynthesisandStructure-ActivityRelationshipsofBenzothienothiazepinoneInhibitorsofProteinKinaseD.
3.BrightbillHD,SutoE,BlaquiereN,RamamoorthiN,Sujatha-BhaskarS,GogolEB,CastanedoGM,JacksonBT,KwonYC,HallerSetal..(2018)NF-κBinducingkinaseisatherapeutictargetforsystemiclupuserythematosus.
4.DavisMI,HuntJP,HerrgardS,CiceriP,WodickaLM,PallaresG,HockerM,TreiberDK,ZarrinkarPP.(2011)Comprehensiveanalysisofkinaseinhibitorselectivity.
5.GaoY,DaviesSP,AugustinM,WoodwardA,PatelUA,KovelmanR,HarveyKJ.(2013)Abroadactivityscreeninsupportofachemogenomicmapforkinasesignallingresearchanddrugdiscovery.
6.GschwendtM,DieterichS,RenneckeJ,KittsteinW,MuellerHJ,JohannesFJ.(1996)InhibitionofproteinkinaseCmubyvariousinhibitors.Differentiationfromproteinkinasecisoenzymes.
7.HarikumarKB,KunnumakkaraAB,OchiN,TongZ,DeorukhkarA,SungB,KellandL,JamiesonS,SutherlandR,RaynhamTetal..(2010)Anovelsmall-moleculeinhibitorofproteinkinaseDblockspancreaticcancergrowthinvitroandinvivo.
8.MeredithEL,ArdayfioO,BeattieK,DoblerMR,EnyedyI,GaulC,HosagraharaV,JewellC,KochK,LeeWetal..(2010)IdentificationoforallyavailablenaphthyridineproteinkinaseDinhibitors.
9.MonovichL,VegaRB,MeredithE,MirandaK,RaoC,CapparelliM,LemonDD,PhanD,KochKA,ChapoJAetal..(2010)AnovelkinaseinhibitorestablishesapredominantroleforproteinkinaseDasacardiacclassIIahistonedeacetylasekinase.
10.WodickaLM,CiceriP,DavisMI,HuntJP,FloydM,SalernoS,HuaXH,FordJM,ArmstrongRC,ZarrinkarPPetal..(2010)Activationstate-dependentbindingofsmallmoleculekinaseinhibitors:structuralinsightsfrombiochemistry.
ProteinkinaseD(PKD)family:proteinkinaseD1.Lastmodifiedon30/05/2018.Accessedon18/05/2020.IUPHAR/BPSGuidetoPHARMACOLOGY,http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1489.