estrogens, progestins, & hormone therapy:estrogens激素治疗,孕激素,和

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1、Estrogens,Progestins,&HormoneTherapyLoreleiVandiverChem5398March25,2008OutlineEstrogensHistorySynthesisReceptorsMedicalUsesProgestinsHistorySynthesisReceptorsMedicalUsesHormoneTherapyMenopauseTypesofHTSteroidSynthesisPicturetakenfromwikipedia.comEstrogensRolesinbothmalesandfemalesMales:growthsp

2、urt,skeletalmaturation,epiphysealclosure,maturationofsperm.Females:developmentoffemalesexorgansandsecondarysexcharacteristics,regulatemenstrualcycle,skeletalmaturationThemostprevalentformsofhumanestrogenareestradiolandestrone.Bothareproducedandsecretedbytheovaries,althoughestroneisalsomadeinthe

3、adrenalglandsandotherorgans.EstrogenHistory1900:Knauerfoundthatovariantransplantspreventsymptomsofgonadectomy.1923:AllenandDoisydevisedabioassayforovarianextracts.1925:Frankandassociatesdetectedanactivesexprincipleinthebloodofsows.1926:LoeweandLangediscoveredthatafemalesexhomonevariedthroughout

4、menstrualcycle.1928:Zondekreportedexcretionofestrogenduringpregnancy.1929:EstrogencrystallizebyButenandtandDoisy1941:FDAapprovalofestrogentherapyformenopausalsymptoms.EstrogenSynthesis-inthebodySynthesisofestrogensmainlyintheovary,bythesynthesisofandrostenedionefromcholesterol.Androstenedioneis

5、thenconvertedtoestroneorestradiol,eitherimmediatelyorthroughtestosterone.Thisprocessiscatalyzedbytheenzymearomatase.EstradiolEstriolEstroneTestosteroneAndrostenedioneAromataseAromataseEstrogenReceptorsEstrogensactassignalingmoleculesbyinteractingwithspecifictargetcells.Includetissuesofthebreast

6、,uterus,brain,heart,liver,andbone.Thesetargetcellshavebindingsitescalledestrogenreceptors.Therearetwoestrogenreceptorsthatarenormallyfoundinthecell’snucleus:ERαandERβ.EstrogenReceptorscont.Thereceptorchangesconformationduetothedissociationofheatshockproteinsafterestrogenbindstoit.Thereceptorund

7、ergoesdimerizationinorderforincreasedaffinitytoDNA.Thisestrogen-receptorcomplexcannowbindtospecificDNAsites,calledestrogenresponseelements(EREs).GenesareactivatedtoproducemessengerRNA,whichguidethesynthesisofnewproteins,determined

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《estrogens, progestins, & hormone therapy:estrogens激素治疗,孕激素,和》由会员上传分享,免费在线阅读,更多相关内容在教育资源-天天文库

1、Estrogens,Progestins,&HormoneTherapyLoreleiVandiverChem5398March25,2008OutlineEstrogensHistorySynthesisReceptorsMedicalUsesProgestinsHistorySynthesisReceptorsMedicalUsesHormoneTherapyMenopauseTypesofHTSteroidSynthesisPicturetakenfromwikipedia.comEstrogensRolesinbothmalesandfemalesMales:growthsp

2、urt,skeletalmaturation,epiphysealclosure,maturationofsperm.Females:developmentoffemalesexorgansandsecondarysexcharacteristics,regulatemenstrualcycle,skeletalmaturationThemostprevalentformsofhumanestrogenareestradiolandestrone.Bothareproducedandsecretedbytheovaries,althoughestroneisalsomadeinthe

3、adrenalglandsandotherorgans.EstrogenHistory1900:Knauerfoundthatovariantransplantspreventsymptomsofgonadectomy.1923:AllenandDoisydevisedabioassayforovarianextracts.1925:Frankandassociatesdetectedanactivesexprincipleinthebloodofsows.1926:LoeweandLangediscoveredthatafemalesexhomonevariedthroughout

4、menstrualcycle.1928:Zondekreportedexcretionofestrogenduringpregnancy.1929:EstrogencrystallizebyButenandtandDoisy1941:FDAapprovalofestrogentherapyformenopausalsymptoms.EstrogenSynthesis-inthebodySynthesisofestrogensmainlyintheovary,bythesynthesisofandrostenedionefromcholesterol.Androstenedioneis

5、thenconvertedtoestroneorestradiol,eitherimmediatelyorthroughtestosterone.Thisprocessiscatalyzedbytheenzymearomatase.EstradiolEstriolEstroneTestosteroneAndrostenedioneAromataseAromataseEstrogenReceptorsEstrogensactassignalingmoleculesbyinteractingwithspecifictargetcells.Includetissuesofthebreast

6、,uterus,brain,heart,liver,andbone.Thesetargetcellshavebindingsitescalledestrogenreceptors.Therearetwoestrogenreceptorsthatarenormallyfoundinthecell’snucleus:ERαandERβ.EstrogenReceptorscont.Thereceptorchangesconformationduetothedissociationofheatshockproteinsafterestrogenbindstoit.Thereceptorund

7、ergoesdimerizationinorderforincreasedaffinitytoDNA.Thisestrogen-receptorcomplexcannowbindtospecificDNAsites,calledestrogenresponseelements(EREs).GenesareactivatedtoproducemessengerRNA,whichguidethesynthesisofnewproteins,determined

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