Aik2|Aim1|AIRK2|ARK2|serine/threonine-proteinkinase12|serine/threonine-proteinkinase5|STK-1|STK12|STK5
Description:HumanAuroraBKinaseincomplexwithINCENPandVX-680(tozasertib)
Downloadallstructure-activitydataforthistargetasaCSVfile

Description:MeasuringphosphorylationofAurBsubstratehistoneH3inA549cells.
Description:Inabiochemicalhomogeneoustime-resolvedfluorescence(HTRF)kinaseassaywithanATPconcentrationof1mM.
EMDMilliporeKinaseProfilerTMscreen/ReactionBiologyKinaseHotspotSMscreen

Ascreenprofiling158kinaseinhibitors(CalbiochemProteinKinaseInhibitorLibraryIandII,cataloguenumbers539744and539745)fortheirinhibitoryactivityat1Mand10Magainst234humanrecombinantkinasesusingtheEMDMilliporeKinaseProfilerTMservice.
Ascreenprofilingtheinhibitoryactivityof178commerciallyavailablekinaseinhibitorsat0.5Magainstapanelof300recombinantproteinkinasesusingtheReactionBiologyCorporationKinaseHotspotSMplatform.
http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx
AurorakinaseB(aspartofthepassengercomplex)localisetocentromeresfromprometaphasetometaphase.Followingchromatidseparation,AurorakinaseBredistributestomidzoneandpersistsatthemidbodyuntilcytokinesisiscompleted.
AurorakinaseBisacomponentofthechromosomalpassengercomplexwhichfunctionstoensureaccuratechromosomesegregationandcellbodydivisionduringmitosis.
1.AdamsND,AdamsJL,BurgessJL,ChaudhariAM,CopelandRA,DonatelliCA,DrewryDH,FisherKE,HamajimaT,HardwickeMAetal..(2010)DiscoveryofGSK1070916,apotentandselectiveinhibitorofAuroraB/Ckinase.
2.Aliagas-MartinI,BurdickD,CorsonL,DotsonJ,DrummondJ,FieldsC,HuangOW,HunsakerT,KleinheinzT,KruegerEetal..(2009)Aclassof2,4-bisanilinopyrimidineAuroraAinhibitorswithunusuallyhighselectivityagainstAuroraB.
3.AnastassiadisT,DeaconSW,DevarajanK,MaH,PetersonJR.(2011)Comprehensiveassayofkinasecatalyticactivityrevealsfeaturesofkinaseinhibitorselectivity.
4.BainJ,PlaterL,ElliottM,ShpiroN,HastieCJ,McLauchlanH,KlevernicI,ArthurJS,AlessiDR,CohenP.(2007)Theselectivityofproteinkinaseinhibitors:afurtherupdate.
5.BarkerMD,LiddleJ,AtkinsonFL,WilsonDM,DicksonMC,Ramirez-MolinaC,LewisH,DavisRP,SomersDO,NeuMetal..(2018)DiscoveryofpotentandselectiveSpleenTyrosineKinaseinhibitorsforthetopicaltreatmentofinflammatoryskindisease.
6.BelangerDB,WilliamsMJ,CurranPJ,MandalAK,MengZ,RainkaMP,YuT,ShihNY,SiddiquiMA,LiuMetal..(2010)Discoveryoforallybioavailableimidazo[1,2-a]pyrazine-basedAurorakinaseinhibitors.
7.BindiS,FancelliD,AlliC,BertaD,BertrandJA,CameronAD,CappellaP,CarpinelliP,CerviG,CrociVetal..(2010)Thieno[3,2-c]pyrazoles:anovelclassofAurorainhibitorswithfavorableantitumoractivity.
8.CurtinML,HeymanHR,FreyRR,MarcottePA,GlaserKB,JankowskiJR,MagocTJ,AlbertDH,OlsonAM,ReuterDRetal..(2012)PyrazolediaminopyrimidinesasdualinhibitorsofKDRandAuroraBkinases.
9.DavisMI,HuntJP,HerrgardS,CiceriP,WodickaLM,PallaresG,HockerM,TreiberDK,ZarrinkarPP.(2011)Comprehensiveanalysisofkinaseinhibitorselectivity.
10.DitchfieldC,JohnsonVL,TigheA,EllstonR,HaworthC,JohnsonT,MortlockA,KeenN,TaylorSS.(2003)AuroraBcoupleschromosomealignmentwithanaphasebytargetingBubR1,Mad2,andCenp-Etokinetochores.
11.ElkinsJM,SantaguidaS,MusacchioA,KnappS.(2012)CrystalstructureofhumanauroraBincomplexwithINCENPandVX-680.
12.FancelliD,MollJ,VarasiM,BravoR,ArticoR,BertaD,BindiS,CameronA,CandianiI,CappellaPetal..(2006)1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles:identificationofapotentAurorakinaseinhibitorwithafavorableantitumorkinaseinhibitionprofile.
13.FedorovO,MarsdenB,PogacicV,RellosP,MüllerS,BullockAN,SchwallerJ,SundströmM,KnappS.(2007)AsystematicinteractionmapofvalidatedkinaseinhibitorswithSer/Thrkinases.
14.FuJ,BianM,JiangQ,ZhangC.(2007)RolesofAurorakinasesinmitosisandtumorigenesis.
15.GaoY,DaviesSP,AugustinM,WoodwardA,PatelUA,KovelmanR,HarveyKJ.(2013)Abroadactivityscreeninsupportofachemogenomicmapforkinasesignallingresearchanddrugdiscovery.
16.GlaserKB,LiJ,MarcottePA,MagocTJ,GuoJ,ReuterDR,TapangP,WeiRQ,PeaseLJ,BuiMHetal..(2012)PreclinicalcharacterizationofABT-348,akinaseinhibitortargetingtheaurora,vascularendothelialgrowthfactorreceptor/platelet-derivedgrowthfactorreceptor,andSrckinasefamilies.
17.HarringtonEA,BebbingtonD,MooreJ,RasmussenRK,Ajose-AdeogunAO,NakayamaT,GrahamJA,DemurC,HercendT,Diu-HercendAetal..(2004)VX-680,apotentandselectivesmall-moleculeinhibitoroftheAurorakinases,suppressestumorgrowthinvivo.
18.HaufS,ColeRW,LaTerraS,ZimmerC,SchnappG,WalterR,HeckelA,vanMeelJ,RiederCL,PetersJM.(2003)ThesmallmoleculeHesperadinrevealsaroleforAuroraBincorrectingkinetochore-microtubuleattachmentandinmaintainingthespindleassemblycheckpoint.
19.HowardS,BerdiniV,BoulstridgeJA,CarrMG,CrossDM,CurryJ,DevineLA,EarlyTR,FazalL,GillALetal..(2009)Fragment-baseddiscoveryofthepyrazol-4-ylurea(AT9283),amultitargetedkinaseinhibitorwithpotentaurorakinaseactivity.
20.JordaR,HendrychováD,VollerJ,ŘezníčkováE,GuckýT,KryštofV.(2018)HowSelectiveArePharmacologicalInhibitorsofCell-Cycle-RegulatingCyclin-DependentKinases?.
21.JungFH,PasquetG,Lambert-vanderBremptC,LohmannJJ,WarinN,RenaudF,GermainH,DeSaviC,RobertsN,JohnsonTetal..(2006)DiscoveryofnovelandpotentthiazoloquinazolinesasselectiveAuroraAandBkinaseinhibitors.
22.LiH,ArgadeA,SinghR,ThotaS,CarrollD,TsoK,TaylorV,MclaughlinJ,MarkovstovVMV.(2005)Cycloalkylsubstitutedpyrimidinediaminecompoundsandtheiruses.
Patentnumber:WO2005118544A2.Assignee:RigelPharmaceuticals,Inc..Prioritydate:18/05/2004.Publicationdate:15/12/2005.23.MedinaJR,BeckerCJ,BlackledgeCW,DuquenneC,FengY,GrantSW,HeerdingD,LiWH,MillerWH,RomerilSPetal..(2011)Structure-baseddesignofpotentandselective3-phosphoinositide-dependentkinase-1(PDK1)inhibitors.
24.MollardA,WarnerSL,CallLT,WadeML,BearssJJ,VermaA,SharmaS,VankayalapatiH,BearssDJ.(2011)Design,SynthesisandBiologicalEvaluationofaSeriesofNovelAxlKinaseInhibitors.
25.OkaniwaM,HiroseM,AritaT,YabukiM,NakamuraA,TakagiT,KawamotoT,UchiyamaN,SumitaA,TsutsumiSetal..(2013)Discoveryofaselectivekinaseinhibitor(TAK-632)targetingpan-RAFinhibition:design,synthesis,andbiologicalevaluationofC-7-substituted1,3-benzothiazolederivatives.
26.OslobJD,RomanowskiMJ,AllenDA,BaskaranS,BuiM,EllingRA,FlanaganWM,FungAD,HananEJ,HarrisSetal..(2008)Discoveryofapotentandselectiveaurorakinaseinhibitor.
27.PaytonM,BushTL,ChungG,ZieglerB,EdenP,McElroyP,RossS,CeeVJ,DeakHL,HodousBLetal..(2010)PreclinicalevaluationofAMG900,anovelpotentandhighlyselectivepan-aurorakinaseinhibitorwithactivityintaxane-resistanttumorcelllines.
28.PollardJR,MortimoreM.(2009)Discoveryanddevelopmentofaurorakinaseinhibitorsasanticanceragents.
29.ShimomuraT,HasakoS,NakatsuruY,MitaT,IchikawaK,KoderaT,SakaiT,NambuT,MiyamotoM,TakahashiIetal..(2010)MK-5108,ahighlyselectiveAurora-Akinaseinhibitor,showsantitumoractivityaloneandincombinationwithdocetaxel.
30.ShiotsuY,KiyoiH,IshikawaY,TanizakiR,ShimizuM,UmeharaH,IshiiK,MoriY,OzekiK,MinamiYetal..(2009)KW-2449,anovelmultikinaseinhibitor,suppressesthegrowthofleukemiacellswithFLT3mutationsorT315I-mutatedBCR/ABLtranslocation.
31.WeïwerM,SpoonamoreJ,WeiJ,GuichardB,RossNT,MassonK,SilkworthW,DandapaniS,PalmerM,SchererCAetal..(2012)APotentandSelectiveQuinoxalinone-BasedSTK33InhibitorDoesNotShowSyntheticLethalityinKRAS-DependentCells.
32.WodickaLM,CiceriP,DavisMI,HuntJP,FloydM,SalernoS,HuaXH,FordJM,ArmstrongRC,ZarrinkarPPetal..(2010)Activationstate-dependentbindingofsmallmoleculekinaseinhibitors:structuralinsightsfrombiochemistry.
33.YangJ,IkezoeT,NishiokaC,TasakaT,TaniguchiA,KuwayamaY,KomatsuN,BandobashiK,TogitaniK,KoefflerHPetal..(2007)AZD1152,anovelandselectiveauroraBkinaseinhibitor,inducesgrowtharrest,apoptosis,andsensitizationfortubulindepolymerizingagentortopoisomeraseIIinhibitorinhumanacuteleukemiacellsinvitroandinvivo.
34.ZhouY,ShanS,LiZB,XinLJ,PanDS,YangQJ,LiuYP,YueXP,LiuXR,GaoJZetal..(2017)CS2164,anovelmulti-targetinhibitoragainsttumorangiogenesis,mitosisandchronicinflammationwithanti-tumorpotency.
Aurorakinase(Aur)family:aurorakinaseB.Lastmodifiedon04/09/2019.Accessedon18/05/2020.IUPHAR/BPSGuidetoPHARMACOLOGY,http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1937.