High-throughput identification of G proteincoupledG蛋白偶聯(lián)物的高通量鑒定 通過(guò)親和質(zhì)量的受體調(diào)節(jié)劑 光譜篩選

《High-throughput identification of G proteincoupledG蛋白偶聯(lián)物的高通量鑒定 通過(guò)親和質(zhì)量的受體調(diào)節(jié)劑 光譜篩選》由會(huì)員上傳分享，免費(fèi)在線閱讀，更多相關(guān)內(nèi)容在學(xué)術(shù)論文-天天文庫(kù)。

1、ChemicalScienceViewArticleOnlineEDGEARTICLEViewJournal

2、ViewIssueHigh-throughputidenti?cationofGprotein-coupledreceptormodulatorsthrougha?nitymassCitethis:Chem.Sci.,2018,9,3192spectrometryscreening?abcbadShanshanQin,?MengmengMeng,?DehuaYang,?WenwenBai,?

3、YanLu,aaaaadeYaoPeng,GaojieSong,YiranWu,QingtongZhou,SuwenZhao,XipingHuang,eccefJohnD.McCorvy,XiaoqingCai,AntaoDai,BryanL.Roth,MichaelA.Hanson,adcdgadadZhi-JieLiu,Ming-WeiWang,*RaymondC.StevensandWenqingShui*Gprotein-coupledreceptors(GPCRs)representthe

4、largestclassofcellsurfaceproteinsandthusconstituteanimportantfamilyoftherapeutictargets.Therefore,signi?cante?orthasbeenputtowardstheidenti?cationofnovelligandsthatcanmodulatetheactivityofaGPCRtargetwithhighe?cacyandselectivity.However,duetolimitations

5、inherenttothemostcommontechniquesforGPCRliganddiscovery,thereisapressingneedformoree?cientande?ectiveligandscreeningmethodsespeciallyCreativeCommonsAttribution3.0UnportedLicence.fortheidenti?cationofpotentialallostericmodulators.Herewepresentahigh-thro

6、ughput,label-freeandunbiasedscreeningapproachfortheidenti?cationofsmallmoleculeligandstowardsGPCRtargetsbasedona?nitymassspectrometry.Thisnewapproachfeaturestheusageoftarget-expressingcellReceived31stOctober2017membranesratherthanpuri?edproteinsforliga

7、ndscreeningandallowsthedetectionofbothAccepted19thFebruary2018orthostericandallostericligandstargetingspeci?cGPCRs.ScreeningasmallcompoundlibrarywiththisDOI:10.1039/c7sc04698gapproachledtotherapiddiscoveryofanantagonistforthe5-HTreceptorandfourpositive

8、allostericrsc.li/chemical-sciencemodulatorsforGLP-1receptorthatwerenotpreviouslyreported.Thisarticleislicensedunderareceptorfunctionalassays,whichmeasureGPCRdownstreamIntroductionsignalinge?ectors,3areinadequateforidentifyingallostericorThesuperfamilyo

9、fG-protein-coupledreceptors(GPCRs)isthebiasedsignalingmodulatorsandoengeneratehitsunsuitableforsubsequentoptimization.4Radioligandbindingassays,largestclassofcellsurfacereceptorsandtheyplayacentralroleOpenAccessArticle.Publishedon20Feb