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1、JournalofSteroidBiochemistry&MolecularBiology137(2013)223–241ContentslistsavailableatScienceDirectJournalofSteroidBiochemistryandMolecularBiologyjournalhomepage:www.elsevier.com/locate/jsbmbReviewProgesteronereceptortargetingwithradiolabelledsteroids:Anap
2、proachinpredictingbreastcancerresponsetotherapySusanaaaaba,?Cunha,LurdesGano,GoretiRibeiroMorais,ThiesThiemann,MariaCristinaOliveiraaUnidadedeCiênciasQuímicaseRadiofarmacêuticas,IST/ITN,InstitutoSuperiorTécnico,UniversidadeTécnicadeLisboa,EstradaNacional1
3、0,2686-953Sacavém,PortugalbFacultyofScience,UnitedArabEmiratesUniversity,UnitedArabEmiratesarticleinfoabstractArticlehistory:SteroidreceptorshavedemonstratedtobepotentiallyusefulbiologicaltargetsforthediagnosisandReceived4December2012therapyfollow-upofhor
4、monallyresponsivecancers.Theover-expressionoftheseproteinsinhumanReceivedinrevisedform24April2013cancercellsaswellastheirbindingcharacteristicsprovidesafavourablemechanismforthelocalization30April2013Acceptedofmalignanttumours.Theneedfornewerandmoreselect
5、iveprobestonon-invasivelyassesssteroidreceptorKeywords:expressioninhormone-responsivetumourshasencouragedthesynthesisandthebiologicalevaluationofseveralsteroidalderivativeslabelledwithpositronandgammaemitters.ThephysiologicalBreastcancereffectsProgesteron
6、eofthesteroidhormoneprogesteronearemediatedbytheprogesteronereceptor(PR).SincePRexpressionisstimulatedbytheoestrogenreceptor(ER),PRstatushasbeenconsideredasabiomarkerofProgesteronereceptorERPETactivityanditsvalueforpredictingandmonitoringtherapeuticef?cac
7、yofhormonaltherapyhasbeenstudied.SPECTImagingofPR-expressingbreastcancerpatientsunderhormonaltherapymaybeadvantageous,sinceImagingtheresponsetotherapycanbemoreaccuratelypredictedafterquanti?cationofbothERandPRTumourtargetingstatus.Thus,ligandsforPRtargeti
8、ng,althoughmuchlessexploredthanERligands,havegainedsomeimportancelatelyaspotentialPETandSPECTtumourimagingagents.Inthisreview,wepresentabriefsurveyofexploredapproachesforprogesteronetargetingusingradiolabelledproges