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1、EuropeanJournalofMedicinalChemistry70(2013)613e622ContentslistsavailableatScienceDirectEuropeanJournalofMedicinalChemistryjournalhomepage:http://www.elsevier.com/locate/ejmechOriginalarticleAdvancesinthestudiesofrolesofRho/Rho-kinaseindiseasesandthedevelopmentofitsinhibitorsa,1a,1a,1aab,*RongguiGua
2、n,XiaoyuXu,MeihuiChen,HaiyanHu,HuGe,ShijunWen,c,*a,*ShiyouZhou,RongbiaoPiaSchoolofPharmaceuticalSciences,SunYat-SenUniversity,Guangzhou510006,ChinabStateKeyLaboratoryofOncologyinSouthChina,SunYat-SenUniversityCancerCenter,Guangzhou510060,ChinacStateKeyLaboratoryofOphthalmology,ZhongshanOphthalmicCe
3、nterofSunYat-SenUniversity,Guangzhou510060,ChinaarticleinfoabstractArticlehistory:RhoA/Rho-kinasepathwayplaysapivotalroleinnumerousfundamentalcellularfunctionsincludingReceived28April2013contraction,motility,proliferation,differentiationandapoptosis.ThepathwayisalsoinvolvedintheReceivedinrevisedfor
4、mdevelopmentofmanydiseasessuchasvasospasm,pulmonaryhypertension,cancerandcentralnervous14October2013systems(CNS)disorders.TheinhibitorsofRhokinasehavebeenextensivelystudiedsincetheRho/Rho-Accepted16October2013kinasepathwaywasverifiedasatargetforanumberofdiseases.Herein,wereviewedtheadvancesinAvailab
5、leonline25October2013thestudiesoftherolesofRho/Rho-kinaseindiseasesandthedevelopmentofRho-kinaseinhibitorsinrecentfiveyears.Keywords:Ó2013ElsevierMassonSAS.Allrightsreserved.RhoARhokinaseInhibitorsCentralnervoussystemFasudil1.Introductionexpressedinmammals,includingRhoA,Rac1,andCdc42.Asthebest-chara
6、cterizedRasprotein,RhoAactsasamolecularswitchRhoisasubfamilymemberofsmallmolecularGTPasessuper-whichcyclesbetweenaninactiveGDP-boundandanactiveGTP-familyrelatedtoRas.Rascomprises20membersandarewidelyboundconformation,interactingwithdownstreamtargetstotriggeraseriesofcellularresponses.TheactivityofR
7、hoAisregu-latedbymanyregulatoryproteins,forexample,guaninenucleotideAbbreviations:ACS,acutecoronarysyndrome;AP-1,activatorprotein-1;AT1,exchangefactors(GEFs),GTPase-activatingproteins(GAPs),andangiotensinII
