RGD Reference Report - Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta. - Rat Genome Database

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Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta.

Authors: Kuiper, GG  Carlsson, B  Grandien, K  Enmark, E  Haggblad, J  Nilsson, S  Gustafsson, JA 
Citation: Kuiper GG, etal., Endocrinology. 1997 Mar;138(3):863-70.
RGD ID: 8694130
Pubmed: PMID:9048584   (View Abstract at PubMed)
DOI: DOI:10.1210/endo.138.3.4979   (Journal Full-text)

The rat estrogen receptor (ER) exists as two subtypes, ER alpha and ER beta, which differ in the C-terminal ligand binding domain and in the N-terminal transactivation domain. In this study we investigated the messenger RNA expression of both ER subtypes in rat tissues by RT-PCR and compared the ligand binding specificity of the ER subtypes. Saturation ligand binding analysis of in vitro synthesized human ER alpha and rat ER beta protein revealed a single binding component for 16 alpha-iodo-17 beta-estradiol with high affinity [dissociation constant (Kd) = 0.1 nM for ER alpha protein and 0.4 nM for ER beta protein]. Most estrogenic substances or estrogenic antagonists compete with 16 alpha-[125I]iodo-17 beta-estradiol for binding to both ER subtypes in a very similar preference and degree; that is, diethylstilbestrol > hexestrol > dienestrol > 4-OH-tamoxifen > 17 beta-estradiol > coumestrol, ICI-164384 > estrone, 17 alpha-estradiol > nafoxidine, moxestrol > clomifene > estriol, 4-OH-estradiol > tamoxifen, 2-OH-estradiol, 5-androstene-3 beta, 17 beta-diol, genistein for the ER alpha protein and dienestrol > 4-OH-tamoxifen > diethylstilbestrol > hexestrol > coumestrol, ICI-164384 > 17 beta-estradiol > estrone, genistein > estriol > nafoxidine, 5-androstene-3 beta, 17 beta-diol > 17 alpha-estradiol, clomifene, 2-OH-estradiol > 4-OH-estradiol, tamoxifen, moxestrol for the ER beta protein. The rat tissue distribution and/or the relative level of ER alpha and ER beta expression seems to be quite different, i.e. moderate to high expression in uterus, testis, pituitary, ovary, kidney, epididymis, and adrenal for ER alpha and prostate, ovary, lung, bladder, brain, uterus, and testis for ER beta. The described differences between the ER subtypes in relative ligand binding affinity and tissue distribution could contribute to the selective action of ER agonists and antagonists in different tissues.



Gene-Chemical Interaction Annotations    Click to see Annotation Detail View

  
Object SymbolSpeciesTermQualifierEvidenceWithNotesSourceOriginal Reference(s)
ESR2Human17alpha-estradiol affects bindingISOEsr2 (Rattus norvegicus)17alpha-estradiol binds to Esr2 proteinRGD 
Esr2Rat17alpha-estradiol affects bindingEXP 17alpha-estradiol binds to Esr2 proteinRGD 
Esr2Mouse17alpha-estradiol affects bindingISOEsr2 (Rattus norvegicus)17alpha-estradiol binds to Esr2 proteinRGD 
ESR2Human17beta-hydroxy-5alpha-androstan-3-one affects bindingISOEsr2 (Rattus norvegicus)5alpha-dihydrotestosterone binds to Esr2 proteinRGD 
Esr2Rat17beta-hydroxy-5alpha-androstan-3-one affects bindingEXP 5alpha-dihydrotestosterone binds to Esr2 proteinRGD 
Esr2Mouse17beta-hydroxy-5alpha-androstan-3-one affects bindingISOEsr2 (Rattus norvegicus)5alpha-dihydrotestosterone binds to Esr2 proteinRGD 
ESR2Human4-Androstenediol affects bindingISOEsr2 (Rattus norvegicus)4-androstenediol binds to Esr2 proteinRGD 
Esr2Rat4-Androstenediol affects bindingEXP 4-androstenediol binds to Esr2 proteinRGD 
Esr2Mouse4-Androstenediol affects bindingISOEsr2 (Rattus norvegicus)4-androstenediol binds to Esr2 proteinRGD 
ESR2Human4-hydroxy-17beta-estradiol affects bindingISOEsr2 (Rattus norvegicus)4-OH-estradiol binds to Esr2 proteinRGD 
Esr2Rat4-hydroxy-17beta-estradiol affects bindingEXP 4-OH-estradiol binds to Esr2 proteinRGD 
Esr2Mouse4-hydroxy-17beta-estradiol affects bindingISOEsr2 (Rattus norvegicus)4-OH-estradiol binds to Esr2 proteinRGD 
ESR2Human5alpha-androstane-3alpha,17beta-diol affects bindingISOEsr2 (Rattus norvegicus)3alpha-androstanediol binds to Esr2 proteinRGD 
Esr2Rat5alpha-androstane-3alpha,17beta-diol affects bindingEXP 3alpha-androstanediol binds to Esr2 proteinRGD 
Esr2Mouse5alpha-androstane-3alpha,17beta-diol affects bindingISOEsr2 (Rattus norvegicus)3alpha-androstanediol binds to Esr2 proteinRGD 
ESR2Human5alpha-androstane-3beta,17beta-diol affects bindingISOEsr2 (Rattus norvegicus)3beta-androstanediol binds to Esr2 proteinRGD 
Esr2Rat5alpha-androstane-3beta,17beta-diol affects bindingEXP 3beta-androstanediol binds to Esr2 proteinRGD 
Esr2Mouse5alpha-androstane-3beta,17beta-diol affects bindingISOEsr2 (Rattus norvegicus)3beta-androstanediol binds to Esr2 proteinRGD 
ESR2Humanbeta-Zearalanol affects bindingISOEsr2 (Rattus norvegicus)Beta-zearalanol binds to Esr2 proteinRGD 
Esr2Ratbeta-Zearalanol affects bindingEXP Beta-zearalanol binds to Esr2 proteinRGD 
Esr2Mousebeta-Zearalanol affects bindingISOEsr2 (Rattus norvegicus)Beta-zearalanol binds to Esr2 proteinRGD 
ESR2Humanclomiphene affects bindingISOEsr2 (Rattus norvegicus)Clomiphene binds to Esr2 proteinRGD 
Esr2Ratclomiphene affects bindingEXP Clomiphene binds to Esr2 proteinRGD 
Esr2Mouseclomiphene affects bindingISOEsr2 (Rattus norvegicus)Clomiphene binds to Esr2 proteinRGD 
ESR2Humancoumestrol affects bindingISOEsr2 (Rattus norvegicus)Coumestrol binds to Esr2 proteinRGD 
Esr2Ratcoumestrol affects bindingEXP Coumestrol binds to Esr2 proteinRGD 
Esr2Ratcoumestrol  IPIcoumestrol RGD 
Esr2Mousecoumestrol affects bindingISOEsr2 (Rattus norvegicus)Coumestrol binds to Esr2 proteinRGD 
ESR2Humandehydroepiandrosterone affects bindingISOEsr2 (Rattus norvegicus)Dehydroepiandrosterone binds to Esr2 proteinRGD 
Esr2Ratdehydroepiandrosterone affects bindingEXP Dehydroepiandrosterone binds to Esr2 proteinRGD 
Esr2Mousedehydroepiandrosterone affects bindingISOEsr2 (Rattus norvegicus)Dehydroepiandrosterone binds to Esr2 proteinRGD 
ESR2Humandienestrol affects bindingISOEsr2 (Rattus norvegicus)Dienestrol binds to Esr2 proteinRGD 
Esr2Ratdienestrol affects bindingEXP Dienestrol binds to Esr2 proteinRGD 
Esr2Mousedienestrol affects bindingISOEsr2 (Rattus norvegicus)Dienestrol binds to Esr2 proteinRGD 
ESR2Humandiethylstilbestrol affects bindingISOEsr2 (Rattus norvegicus)Diethylstilbestrol binds to Esr2 proteinRGD 
Esr2Ratdiethylstilbestrol affects bindingEXP Diethylstilbestrol binds to Esr2 proteinRGD 
Esr2Mousediethylstilbestrol affects bindingISOEsr2 (Rattus norvegicus)Diethylstilbestrol binds to Esr2 proteinRGD 
ESR2Humanestriol affects bindingISOEsr2 (Rattus norvegicus)Estriol binds to Esr2 proteinRGD 
Esr2Ratestriol affects bindingEXP Estriol binds to Esr2 proteinRGD 
Esr2Mouseestriol affects bindingISOEsr2 (Rattus norvegicus)Estriol binds to Esr2 proteinRGD 
ESR2Humanestrone affects bindingISOEsr2 (Rattus norvegicus)Estrone binds to Esr2 proteinRGD 
Esr2Ratestrone affects bindingEXP Estrone binds to Esr2 proteinRGD 
Esr2Mouseestrone affects bindingISOEsr2 (Rattus norvegicus)Estrone binds to Esr2 proteinRGD 
ESR2Humanestrone 3-sulfate affects bindingISOEsr2 (Rattus norvegicus)Estrone-3-sulfate binds to Esr2 proteinRGD 
Esr2Ratestrone 3-sulfate affects bindingEXP Estrone-3-sulfate binds to Esr2 proteinRGD 
Esr2Mouseestrone 3-sulfate affects bindingISOEsr2 (Rattus norvegicus)Estrone-3-sulfate binds to Esr2 proteinRGD 
ESR2Humangenistein affects bindingISOEsr2 (Rattus norvegicus)Genistein binds to Esr2 proteinRGD 
Esr2Ratgenistein affects bindingEXP Genistein binds to Esr2 proteinRGD 
Esr2Mousegenistein affects bindingISOEsr2 (Rattus norvegicus)Genistein binds to Esr2 proteinRGD 
ESR2Humanhexestrol affects bindingISOEsr2 (Rattus norvegicus)Hexestrol binds to Esr2 proteinRGD 
Esr2Rathexestrol affects bindingEXP Hexestrol binds to Esr2 proteinRGD 
Esr2Mousehexestrol affects bindingISOEsr2 (Rattus norvegicus)Hexestrol binds to Esr2 proteinRGD 
ESR2Humanmethoxychlor affects bindingISOEsr2 (Rattus norvegicus)Methoxychlor binds to Esr2 proteinRGD 
Esr2Ratmethoxychlor affects bindingEXP Methoxychlor binds to Esr2 proteinRGD 
Esr2Mousemethoxychlor affects bindingISOEsr2 (Rattus norvegicus)Methoxychlor binds to Esr2 proteinRGD 
ESR2HumanMoxestrol affects bindingISOEsr2 (Rattus norvegicus)Moxestrol binds to Esr2 proteinRGD 
Esr2RatMoxestrol affects bindingEXP Moxestrol binds to Esr2 proteinRGD 
Esr2MouseMoxestrol affects bindingISOEsr2 (Rattus norvegicus)Moxestrol binds to Esr2 proteinRGD 
ESR2Humannandrolone affects bindingISOEsr2 (Rattus norvegicus)19-nortestosterone binds to Esr2 proteinRGD 
Esr2Ratnandrolone affects bindingEXP 19-nortestosterone binds to Esr2 proteinRGD 
Esr2Mousenandrolone affects bindingISOEsr2 (Rattus norvegicus)19-nortestosterone binds to Esr2 proteinRGD 
ESR2HumanNorethynodrel affects bindingISOEsr2 (Rattus norvegicus)Norethynodrel binds to Esr2 proteinRGD 
Esr2RatNorethynodrel affects bindingEXP Norethynodrel binds to Esr2 proteinRGD 
Esr2MouseNorethynodrel affects bindingISOEsr2 (Rattus norvegicus)Norethynodrel binds to Esr2 proteinRGD 
ESR2Humantamoxifen affects bindingISOEsr2 (Rattus norvegicus)Tamoxifen binds to Esr2 proteinRGD 
Esr2Rattamoxifen affects bindingEXP Tamoxifen binds to Esr2 proteinRGD 
Esr2Mousetamoxifen affects bindingISOEsr2 (Rattus norvegicus)Tamoxifen binds to Esr2 proteinRGD 

Gene Ontology Annotations    Click to see Annotation Detail View

Molecular Function

  

Objects Annotated

Genes (Rattus norvegicus)
Esr2  (estrogen receptor 2)

Genes (Mus musculus)
Esr2  (estrogen receptor 2 (beta))

Genes (Homo sapiens)
ESR2  (estrogen receptor 2)


Additional Information