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FYN protooncogene, Src family tyrosine kinase | Src family | IUPHAR/BPS Guide to PHARMACOLOGY188bio精品生物—专注于实验室精品爆款的电商平台 - 蚂蚁淘旗下精选188款生物医学科研用品
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FYN protooncogene, Src family tyrosine kinase | Src family | IUPHAR/BPS Guide to PHARMACOLOGY

FGR|p59-Fyn|SLK|SrcKinasep59|SYN|FYNoncogenerelatedtoSRC,FGR,YES|FYNproto-oncogene
Description:CrystalStructureofFynkinasedomaincomplexedwithstaurosporine
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
AnimalmodelsandcelllinestudiesindicateacriticalroleforFyninproximalT-cellantigenreceptor(TCR)signaltransduction[13].TCR-basedsignalsarerequiredatseveralstagesofT-celldevelopment.NotethatisthoughtthattherelatedSrctyrosinekinaseLckisthemajorcontributortoTCRsignaltransduction.
1.AnastassiadisT,DeaconSW,DevarajanK,MaH,PetersonJR.(2011)Comprehensiveassayofkinasecatalyticactivityrevealsfeaturesofkinaseinhibitorselectivity.
2.BachegowdaL,MorroneK,WinskiSL,MantzarisI,BartensteinM,RamachandraN,GiriczO,SukrithanV,NwankwoG,ShahnazSetal..(2016)Pexmetinib:ANovelDualInhibitorofTie2andp38MAPKwithEfficacyinPreclinicalModelsofMyelodysplasticSyndromesandAcuteMyeloidLeukemia.
3.BarfTA,JansCGJM,ManPADeA,OubrieAA,RaaijmakersHCA,RewinkelJBM,SterrenburgJ-G,WijkmansJCHM.(2014)4-imidazopyridazin-1-yl-benzamidesand4-imidazotriazin-1-yl-benzamidesasbtkinhibitors.
Patentnumber:US20140155385A1.Assignee:BarfTA,JansCGJM,ManPADeA,OubrieAA,RaaijmakersHCA,RewinkelJBM,SterrenburgJ-G,WijkmansJCHM.Prioritydate:19/07/2011.Publicationdate:05/06/2014.4.ByrdJC,HarringtonB,O"BrienS,JonesJA,SchuhA,DevereuxS,ChavesJ,WierdaWG,AwanFT,BrownJRetal..(2016)Acalabrutinib(ACP-196)inRelapsedChronicLymphocyticLeukemia.
5.ChenP,NorrisD,DasJ,SpergelSH,WityakJ,LeithL,ZhaoR,ChenBC,PittS,PangSetal..(2004)Discoveryofnovel2-(aminoheteroaryl)-thiazole-5-carboxamidesaspotentandorallyactiveSrc-familykinasep56(Lck)inhibitors.
6.DavisMI,HuntJP,HerrgardS,CiceriP,WodickaLM,PallaresG,HockerM,TreiberDK,ZarrinkarPP.(2011)Comprehensiveanalysisofkinaseinhibitorselectivity.
7.FraserC,DawsonJC,DowlingR,HoustonDR,WeissJT,MunroAF,MuirM,HarringtonL,WebsterSP,FrameMCetal..(2016)RapidDiscoveryandStructure-ActivityRelationshipsofPyrazolopyrimidinesThatPotentlySuppressBreastCancerCellGrowthviaSRCKinaseInhibitionwithExceptionalSelectivityoverABLKinase.
8.GaoY,DaviesSP,AugustinM,WoodwardA,PatelUA,KovelmanR,HarveyKJ.(2013)Abroadactivityscreeninsupportofachemogenomicmapforkinasesignallingresearchanddrugdiscovery.
9.HankeJH,GardnerJP,DowRL,ChangelianPS,BrissetteWH,WeringerEJ,PollokBA,ConnellyPA.(1996)Discoveryofanovel,potent,andSrcfamily-selectivetyrosinekinaseinhibitor.StudyofLck-andFynT-dependentTcellactivation.
10.KinoshitaT,MatsubaraM,IshiguroH,OkitaK,TadaT.(2006)StructureofhumanFynkinasedomaincomplexedwithstaurosporine.
11.LowellCA.(2004)Src-familykinases:rheostatsofimmunecellsignaling.
12.Martin-GarciaJM,LuqueI,Ruiz-SanzJ,Camara-ArtigasA.(2012)ThepromiscuousbindingoftheFynSH3domaintoapeptidefromtheNS5Aprotein.
13.PalaciosEH,WeissA.(2004)FunctionoftheSrc-familykinases,LckandFyn,inT-celldevelopmentandactivation.
14.RemsingRixLL,RixU,ColingeJ,HantschelO,BennettKL,StranzlT,MüllerA,BaumgartnerC,ValentP,AugustinMetal..(2009)Globaltargetprofileofthekinaseinhibitorbosutinibinprimarychronicmyeloidleukemiacells.
15.WodickaLM,CiceriP,DavisMI,HuntJP,FloydM,SalernoS,HuaXH,FordJM,ArmstrongRC,ZarrinkarPPetal..(2010)Activationstate-dependentbindingofsmallmoleculekinaseinhibitors:structuralinsightsfrombiochemistry.
16.YaoX,SunX,JinS,YangL,XuH,RaoY.(2019)Discoveryof4-Aminoquinoline-3-carboxamideDerivativesasPotentReversibleBruton"sTyrosineKinaseInhibitorsfortheTreatmentofRheumatoidArthritis.
Srcfamily:FYNproto-oncogene,Srcfamilytyrosinekinase.Lastmodifiedon16/07/2019.Accessedon18/05/2020.IUPHAR/BPSGuidetoPHARMACOLOGY,http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2026.

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