Progesterone receptor targeting with radiolabelled steroids An approach in predicting breast cancer response to therapy

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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),PRstatushasbeenconsideredasabiomarkerofProgesteronereceptorERPETactivityanditsvalueforpredictingandmonitoringtherapeuticefficac

7、yofhormonaltherapyhasbeenstudied.SPECTImagingofPR-expressingbreastcancerpatientsunderhormonaltherapymaybeadvantageous,sinceImagingtheresponsetotherapycanbemoreaccuratelypredictedafterquantificationofbothERandPRTumourtargetingstatus.Thus,ligandsforPRtargeti

8、ng,althoughmuchlessexploredthanERligands,havegainedsomeimportancelatelyaspotentialPETandSPECTtumourimagingagents.Inthisreview,wepresentabriefsurveyofexploredapproachesforprogesteronetargetingusingradiolabelledproges