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1、NIHPublicAccessAuthorManuscriptScience.Authormanuscript;availableinPMC2008November23.NIH-PAAuthorManuscriptPublishedinfinaleditedformas:NIH-PAAuthorManuscriptNIH-PAAuthorManuscriptScience.2007November23;318(5854):1258±1265.doi:10.1126/science.1150577.HighResolutionCrystalStructureofan
2、EngineeredHumanβ2-AdrenergicGprotein-CoupledReceptorVadimCherezov1,$,DanielM.Rosenbaum2,$,MichaelA.Hanson1,SørenG.F.Rasmussen2,FoonSunThian2,TongSunKobilka2,Hee-JungChoi2,3,PeterKuhn4,WilliamI.Weis2,3,BrianK.Kobilka2,*,andRaymondC.Stevens1,*1DepartmentofMolecularBiology,TheScrippsRese
3、archInstitute,LaJolla,CA,92037USA2DepartmentofMolecularandCellularPhysiology,StanfordUniversitySchoolofMedicine,Stanford,CA94305USA3DepartmentofStructuralBiology,StanfordUniversitySchoolofMedicine,Stanford,CA94305USA4DepartmentofCellBiology,TheScrippsResearchInstitute,LaJolla,CA,92037
4、USAAbstractGprotein-coupledreceptorscomprisethelargestfamilyofeukaryoticsignaltransductionproteinsthatcommunicateacrossthemembrane.Wereportthecrystalstructureofahumanβ2-adrenergicreceptor—T4lysozymefusionproteinboundtothepartialinverseagonistcarazololat2.4Åresolution.Thestructureprovi
5、desahigh-resolutionviewofahumanGprotein-coupledreceptorboundtoadiffusibleligand.Ligand-bindingsiteaccessibilityisenabledbythesecondextracellularloopwhichisheldoutofthebindingcavitybyapairofcloselyspaceddisulfidebridgesandashorthelicalsegmentwithintheloop.Cholesterol,anecessarycomponen
6、tforcrystallization,mediatesanintriguingparallelassociationofreceptormoleculesinthecrystallattice.Althoughthelocationofcarazololintheβ2-adrenergicreceptorisverysimilartothatofretinalinrhodopsin,structuraldifferencesintheligandbindingsiteandotherregionshighlightthechallengesinusingrhod
7、opsinasatemplatemodelforthislargereceptorfamily.*Towhomcorrespondenceshouldbeaddressed:stevens@scripps.edu;kobilka@stanford.edu$TheseauthorscontributedequallyAuthorContributions:RCSandBKKindependentlypushedtheGPCRstructuralbiologyprojectsformorethan15years.BKKmanagedtheproteindesign,p
8、roduc
