Targeting the androgen receptor in prostate cancer

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1、ReviewTargetingtheandrogenreceptorinprostatecancerZoranCulig1.IntroductionInnsbruckMedicalUniversity,ExperimentalUrology,DepartmentofUrology,Innsbruck,Austria2.Nonsteroidalanti-androgensIntroduction:Theandrogenreceptor(AR)isaligand-activatedtranscript

2、ionhydroxyflutamideandfactorthatisexpressedinprimaryandmetastaticprostatecancers.TherebicalutamideinprostateareadvancesinendocrinetherapyforprostatecancerthatarebasedoncancertreatmentimprovedunderstandingofARfunction.3.ProstatecancercelllinesasaAreasc

3、overed:PubMedhasbeenusedtoincludemostimportantpublicationsmodelforevaluationofontargetingtheARinprostatecancer.ARexpressionmaybedownregulatedeffectsofchemopreventivebyagentsusedforchemopreventionofprostatecanceror,inmodelsofagentsadvancedprostatecance

4、r,byantisenseoligonucleotides.Newdrugsthat4.InhibitionofARbyantisenseinhibitthesteroidogenicenzymeCYP17A1(abirateroneacetate)ordiminisholigonucleotidesandnucleartranslocationoftheAR(enzalutamide)havebeenshowntoimproveneutralizingantibodiespatients’sur

5、vivalinprostatecancer.However,itisclearthatthereisadevel-5.TargetingARcoactivatorsopmentofresistancetothesenoveltherapies.Theymayincludeincreased6.Dualeffectsofanti-estrogensexpressionoftruncated,constitutivelyactiveARoractivationofthesignalinginhuman

6、prostatecancerpathwayofsignaltransducersandactivatorsoftranscription.Expertopinion:Althoughintroductionofnoveldrugshaveimproved7.InhibitionofCYP17A1enzymeinprostatecancerpatients’survival,thereisaneedtoinvestigatethemechanismsofresistancefurther.Thero

7、leoftruncatedARandcompensatoryactivationofsignaling8.Heat-shockproteinpathwaysaswellasthedevelopmentofscientificallyjustifiedcombination90inhibitorsandhistonetherapiesseemstobeissuesofahighpriority.deacetylaseinhibitorsinprostatecancerKeywords:androge

8、nreceptor,chemotherapy,prostatecancer,steroidogenesis9.ApplicationofASC-J9inhumanprostatecancerExpertOpin.Pharmacother.[EarlyOnline]10.EffectsofchemotherapeuticsonARsignalinginprostate1.IntroductioncancerTraditionally,treatmentofprostatecancer