Voltage-DependentBlockofN-Methyl-D-aspartateReceptorsbyDopamineD1ReceptorLigands
...mulatingevidenceindicatesthatdopamineandD1receptorligandsmodulateN-methylD-aspartate(NMDA)receptorsthroughavarietyofD1receptor-dependentmechanisms.Inthisstudy,werevealadistinctD1receptor-independentmechanismbywhichNMDAreceptorsaremodulated.Usingthehumanembryonickidney(HEK)cellrecombinantsystemanddis...
醫源資料庫;在線期刊;分子藥理學雜誌;2006年第68卷第11期StructuralDeterminatesforApolipoproteinE-DerivedPeptideInteractionwiththe7NicotinicAcetylcholineReceptor
....ThepercentageblockbyapoE141–148isforasingleconcentrationof3µM.Aspreviouslyreported(Gayetal.,2006),theeight-amino-acidpeptideapoE141–148(3µM,nearmaximalinhibition)significantlyreducedtheamplitudeofwild-type7nAChR-mediatedresponsesby78±3%(Table1,Fig.2A).Itisnoteworthyth...
醫源資料庫;在線期刊;分子藥理學雜誌;2007年第69卷第10期SerineproteaseHtrA1modulateschemotherapy-inducedcytotoxicity
...9).WehavepreviouslyshownthatforcedexpressionofWTHtrA1inducedcelldeath,whereasprotease-inactivemutant(S328A)HtrA1failedtoinducecelldeath,indicatingthatserineproteaseactivityinHtrA1isimportantforitsproapoptoticproperty(16).Similarly,severalreportshavepreviouslydemonstratedthatacloselyrelatedprotease,H...
醫源資料庫;在線期刊;臨牀研究雜誌;2006年第116卷第7期MultipleBindingSitesforSubstratesandModulatorsofSemicarbazide-SensitiveAmineOxidases:KineticConsequences
...siduesclosetothetopaquinone(TPQ)cofactorandinasecondaryanioniccavityclosetoAsp445‘,onahairpinloopextendingfromtheopposingmonomer,approximately10ÅfromTPQ(DiPaoloetal.,2003).Tetraphenylphosphonium(TPP+),aninhibitortoolargetoaccesstheBPAOactivesite,isabletoinhibitoxidationofbothSPDandbenzylamin...
醫源資料庫;在線期刊;分子藥理學雜誌;2008年第70卷第2期Shigatoxin-InducedEndothelin-ExpressioninCulturedPodocytesAutocrinallyMediatesActinRemodeling
...Mundel,DepartmentofMedicine,MountSinaiSchoolofMedicine,NewYork,NY)weregrownaspreviouslydescribed.19Briefly,cellswereculturedundergrowth-permissiveconditionsonrattailcollagentypeI-coatedplasticdishes(BDBioscience,Bedford,MA)at33??CinRPMI1640(Invitrogen,Gaithersburg,MD)supplementedwith10%fetalbovinese...
醫源資料庫;在線期刊;美國病理學雜誌;2006年第168卷第12期NeuropeptideFF(NPFF)AnalogsFunctionallyAntagonizeOpioidActivitiesinNPFF2Receptor-TransfectedSH-SY5YNeuroblastomaCells
...on(Harrisonetal.,1998;RoumyandZajac,1998;Panulaetal.,1999).Forinstance,supraspinalinjectionofNPFFanalogs,whichhaslittleornoeffectinpaintests,decreasesmorphine-inducedanalgesia(antiopioidactivity,RoumyandZajac,1998;Panulaetal.,1999),whereasspinaladministrationinducesanaloxone-sensitiveanalgesiaandpot...
醫源資料庫;在線期刊;分子藥理學雜誌;2005年第67卷第3期N-(6-Chloro-pyridin-3-yl)-3,4-difluoro-benzamide(ICA-27243):ANovel,SelectiveKCNQ2/Q3PotassiumChannelActivator
...ietal.,1984;Aikenetal.,1995).Collectively,thesedataidentifyKCNQ2/Q3channelsaspotentiallyattractivetargetsformechanisticallynovelAEDsandsuggestthatagentscapableofselectivelyenhancingtheactivationofKCNQ2/Q3channelsmayrepresentnovelanticonvulsantdrugs.Fig.1.ICA-27243isstructurallydistinctfromotherknown...
醫源資料庫;在線期刊;分子藥理學雜誌;2008年第70卷第3期ConformationalConstrainingofInactiveandActiveStatesofaSevenTransmembraneReceptorbyMetalIonSiteEngineeringintheExtracellularEndofTransmem
...0werefromPeprotech(RockyHill,NJ).Otherhumanchemokinesweremadein-housebyThomasP.BoesenthroughEscherichiacoliexpression,purification,andrefolding(CXCL8/IL8)orbyCOS-7cellexpression,purification,andrefolding(vCCL2)(Kledaletal.,1997).ORF74-HHV8(Genbankaccessionno.U24275)wasclonedfromaKaposi‘ssarcomaski...
醫源資料庫;在線期刊;分子藥理學雜誌;2006年第68卷第12期InsightsintotheCholecystokinin2ReceptorBindingSiteandProcessesofActivation
...hendemonstratedthatHis207inECL2oftheCCK2RinteractsdirectlywiththeC-terminalAsp8ofCCK(Silvente-Poirotetal.,1999).Basedonthesedifferentresults,weestablishedamolecularmodeloftheCCK2RoccupiedbyCCK.Thismodelenabledustoidentifytwonewresiduesnotidentifiedbymutagenesis,Tyr189(Y4.60)andAsn358(N6.55),inintera...
醫源資料庫;在線期刊;分子藥理學雜誌;2006年第68卷第12期ThiazolidinedionesModulatetheExpressionof-CateninandOtherCell-CycleRegulatoryProteinsbyTargetingtheF-BoxProteinsofSkp1-Cul1-F-boxProteinE3
...andFbw7,therebyaffectingmanyofthetargetproteinsofthesetwoF-boxproteins(suchasp27andcyclinE).Asaconsequence,theabilityoftroglitazonetotargettheseF-boxproteinsprovidesamolecularbasistoaccountforitsreportedeffectonmodulatingtheexpressionofaforementionedcell-cycleregulatoryproteins.Despitethiscomplicate...
醫源資料庫;在線期刊;分子藥理學雜誌;2007年第69卷第9期