A Small Molecule Agonist of EphA2 Receptor Tyrosine Kinase Inhibits Tumor Cell Migration In Vitro and Prostate Cancer Metastasis In Vivo 英文参考文献.docVIP
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A Small Molecule Agonist of EphA2 Receptor Tyrosine Kinase Inhibits Tumor Cell Migration In Vitro and Prostate Cancer Metastasis In Vivo 英文参考文献
ASmallMoleculeAgonistofEphA2ReceptorTyrosine
KinaseInhibitsTumorCellMigrationInVitroand
ProstateCancerMetastasisInVivo
AaronPetty1.,EugeneMyshkin1.,HainaQin2.,HongGuo1,HuiMiao1,GregoryP.Tochtrop3,4 ,Jer-
TsongHsieh5,PhillipPage6,LiliLiu7,DanielJ.Lindner8,ChayanAcharya9,AlexanderD.MacKerell Jr.9,
EckhardFicker1,JianxingSong2,10*,BingchengWang1,4,11
*
1RammelkampCenterforResearchandDepartmentofMedicine,MetroHealthCampus,CaseWesternReserveUniversitySchoolofMedicine,Cleveland,Ohio,United
States ofAmerica, 2Departments ofBiological Sciences, Faculty ofScience, National University ofSingapore,Singapore, Singapore, 3Department ofChemistry, Case
Western Reserve University, Cleveland, Ohio, United States of America, 4Case Comprehensive Cancer Center, Case Western Reserve University School of Medicine,
Cleveland,Ohio,UnitedStatesofAmerica,5DepartmentofUrology,UniversityofTexasSouthwesternMedicalCenter,Dallas,Texas,UnitedStatesofAmerica,6Reichert,
Inc., Depew, New York, United States of America, 7Department of Medicine, Division of Hematology and Oncology, University Hospitals Case Medical Center, Case
WesternReserveUniversitySchoolofMedicine,Cleveland,Ohio,UnitedStatesofAmerica,8TaussigCancerInstitute,ClevelandClinicFoundation,Cleveland,Ohio,United
StatesofAmerica,9DepartmentofPharmaceuticalSciences,SchoolofPharmacy,UniversityofMaryland,Baltimore,Maryland,UnitedStatesofAmerica,10Department
of Biochemistry, Yong Loo Lin School of Medicine, National University of Singapore, Singapore, Singapore, 11Department of Pharmacology, Case Western Reserve
UniversitySchoolofMedicine,Cleveland,Ohio,UnitedStatesofAmerica
Abstract
Duringtumorprogression,EphA2receptorcangainligand-independentpro-oncogenicfunctionsduetoAktactivationand
reducedephrin-Aligandengagement.Theeffectscanbereversedbyligandstimulation,whichtriggerstheintrinsictumor
suppressivesignalingpathwaysofEphA2includinginhibitionofPI3/AktandRas/ERKpathways.Theseobservationsargue
fordevelopmentofsmallmoleculeagonistsforEp
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