Estrogen receptor

Details

Name
Estrogen receptor
Synonyms
  • ER
  • ER-alpha
  • ESR
  • Estradiol receptor
  • NR3A1
  • Nuclear receptor subfamily 3 group A member 1
Gene Name
ESR1
Organism
Humans
Amino acid sequence
>lcl|BSEQ0000246|Estrogen receptor
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAY
EFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPF
LQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAK
ETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQAC
RLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKR
SKKNSLALSLTADQMVSALLDAEPPILYSEYDPTRPFSEASMMGLLTNLADRELVHMINW
AKRVPGFVDLTLHDQVHLLECAWLEILMIGLVWRSMEHPGKLLFAPNLLLDRNQGKCVEG
MVEIFDMLLATSSRFRMMNLQGEEFVCLKSIILLNSGVYTFLSSTLKSLEEKDHIHRVLD
KITDTLIHLMAKAGLTLQQQHQRLAQLLLILSHIRHMSNKGMEHLYSMKCKNVVPLYDLL
LEMLDAHRLHAPTSRGGASVEETDQSHLATAGSTSSHSLQKYYITGEAEGFPATV
Number of residues
595
Molecular Weight
66215.45
Theoretical pI
8.14
GO Classification
Functions
ATPase binding / beta-catenin binding / chromatin binding / core promoter sequence-specific DNA binding / enzyme binding / estrogen receptor activity / estrogen response element binding / identical protein binding / nitric-oxide synthase regulator activity / RNA polymerase II core promoter proximal region sequence-specific DNA binding / RNA polymerase II transcription factor activity, estrogen-activated sequence-specific DNA binding / steroid binding / steroid hormone receptor activity / transcription factor activity, sequence-specific DNA binding / transcription factor binding / transcriptional activator activity, RNA polymerase II core promoter proximal region sequence-specific binding / zinc ion binding
Processes
androgen metabolic process / antral ovarian follicle growth / cellular response to estradiol stimulus / chromatin remodeling / epithelial cell development / epithelial cell proliferation involved in mammary gland duct elongation / gene expression / intracellular estrogen receptor signaling pathway / intracellular steroid hormone receptor signaling pathway / male gonad development / mammary gland alveolus development / mammary gland branching involved in pregnancy / negative regulation of gene expression / negative regulation of I-kappaB kinase/NF-kappaB signaling / negative regulation of sequence-specific DNA binding transcription factor activity / phospholipase C-activating G-protein coupled receptor signaling pathway / positive regulation of cytosolic calcium ion concentration / positive regulation of fibroblast proliferation / positive regulation of nitric oxide biosynthetic process / positive regulation of nitric-oxide synthase activity / positive regulation of phospholipase C activity / positive regulation of sequence-specific DNA binding transcription factor activity / positive regulation of transcription from RNA polymerase II promoter / positive regulation of transcription, DNA-templated / prostate epithelial cord arborization involved in prostate glandular acinus morphogenesis / prostate epithelial cord elongation / regulation of apoptotic process / regulation of branching involved in prostate gland morphogenesis / regulation of transcription, DNA-templated / response to estradiol / response to estrogen / signal transduction / transcription from RNA polymerase II promoter / transcription initiation from RNA polymerase II promoter / transcription, DNA-templated / uterus development / vagina development
Components
cytoplasm / cytosol / Golgi apparatus / integral component of membrane / membrane / nuclear chromatin / nucleoplasm / nucleus / plasma membrane / transcriptionally active chromatin
General Function
Zinc ion binding
Specific Function
Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Ligand-dependent nuclear transactivation involves either direct homodimer binding to a palindromic estrogen response element (ERE) sequence or association with other DNA-binding transcription factors, such as AP-1/c-Jun, c-Fos, ATF-2, Sp1 and Sp3, to mediate ERE-independent signaling. Ligand binding induces a conformational change allowing subsequent or combinatorial association with multiprotein coactivator complexes through LXXLL motifs of their respective components. Mutual transrepression occurs between the estrogen receptor (ER) and NF-kappa-B in a cell-type specific manner. Decreases NF-kappa-B DNA-binding activity and inhibits NF-kappa-B-mediated transcription from the IL6 promoter and displace RELA/p65 and associated coregulators from the promoter. Recruited to the NF-kappa-B response element of the CCL2 and IL8 promoters and can displace CREBBP. Present with NF-kappa-B components RELA/p65 and NFKB1/p50 on ERE sequences. Can also act synergistically with NF-kappa-B to activate transcription involving respective recruitment adjacent response elements; the function involves CREBBP. Can activate the transcriptional activity of TFF1. Also mediates membrane-initiated estrogen signaling involving various kinase cascades. Isoform 3 is involved in activation of NOS3 and endothelial nitric oxide production. Isoforms lacking one or several functional domains are thought to modulate transcriptional activity by competitive ligand or DNA binding and/or heterodimerization with the full length receptor. Essential for MTA1-mediated transcriptional regulation of BRCA1 and BCAS3. Isoform 3 can bind to ERE and inhibit isoform 1.
Pfam Domain Function
Transmembrane Regions
Not Available
Cellular Location
Nucleus
Gene sequence
>lcl|BSEQ0021831|Estrogen receptor (ESR1)
ATGACCATGACCCTCCACACCAAAGCATCTGGGATGGCCCTACTGCATCAGATCCAAGGG
AACGAGCTGGAGCCCCTGAACCGTCCGCAGCTCAAGATCCCCCTGGAGCGGCCCCTGGGC
GAGGTGTACCTGGACAGCAGCAAGCCCGCCGTGTACAACTACCCCGAGGGCGCCGCCTAC
GAGTTCAACGCCGCGGCCGCCGCCAACGCGCAGGTCTACGGTCAGACCGGCCTCCCCTAC
GGCCCCGGGTCTGAGGCTGCGGCGTTCGGCTCCAACGGCCTGGGGGGTTTCCCCCCACTC
AACAGCGTGTCTCCGAGCCCGCTGATGCTACTGCACCCGCCGCCGCAGCTGTCGCCTTTC
CTGCAGCCCCACGGCCAGCAGGTGCCCTACTACCTGGAGAACGAGCCCAGCGGCTACACG
GTGCGCGAGGCCGGCCCGCCGGCATTCTACAGGCCAAATTCAGATAATCGACGCCAGGGT
GGCAGAGAAAGATTGGCCAGTACCAATGACAAGGGAAGTATGGCTATGGAATCTGCCAAG
GAGACTCGCTACTGTGCAGTGTGCAATGACTATGCTTCAGGCTACCATTATGGAGTCTGG
TCCTGTGAGGGCTGCAAGGCCTTCTTCAAGAGAAGTATTCAAGGACATAACGACTATATG
TGTCCAGCCACCAACCAGTGCACCATTGATAAAAACAGGAGGAAGAGCTGCCAGGCCTGC
CGGCTCCGCAAATGCTACGAAGTGGGAATGATGAAAGGTGGGATACGAAAAGACCGAAGA
GGAGGGAGAATGTTGAAACACAAGCGCCAGAGAGATGATGGGGAGGGCAGGGGTGAAGTG
GGGTCTGCTGGAGACATGAGAGCTGCCAACCTTTGGCCAAGCCCGCTCATGATCAAACGC
TCTAAGAAGAACAGCCTGGCCTTGTCCCTGACGGCCGACCAGATGGTCAGTGCCTTGTTG
GATGCTGAGCCCCCCATACTCTATTCCGAGTATGATCCTACCAGACCCTTCAGTGAAGCT
TCGATGATGGGCTTACTGACCAACCTGGCAGACAGGGAGCTGGTTCACATGATCAACTGG
GCGAAGAGGGTGCCAGGCTTTGTGGATTTGACCCTCCATGATCAGGTCCACCTTCTAGAA
TGTGCCTGGCTAGAGATCCTGATGATTGGTCTCGTCTGGCGCTCCATGGAGCACCCAGGG
AAGCTACTGTTTGCTCCTAACTTGCTCTTGGACAGGAACCAGGGAAAATGTGTAGAGGGC
ATGGTGGAGATCTTCGACATGCTGCTGGCTACATCATCTCGGTTCCGCATGATGAATCTG
CAGGGAGAGGAGTTTGTGTGCCTCAAATCTATTATTTTGCTTAATTCTGGAGTGTACACA
TTTCTGTCCAGCACCCTGAAGTCTCTGGAAGAGAAGGACCATATCCACCGAGTCCTGGAC
AAGATCACAGACACTTTGATCCACCTGATGGCCAAGGCAGGCCTGACCCTGCAGCAGCAG
CACCAGCGGCTGGCCCAGCTCCTCCTCATCCTCTCCCACATCAGGCACATGAGTAACAAA
GGCATGGAGCATCTGTACAGCATGAAGTGCAAGAACGTGGTGCCCCTCTATGACCTGCTG
CTGGAGATGCTGGACGCCCACCGCCTACATGCGCCCACTAGCCGTGGAGGGGCATCCGTG
GAGGAGACGGACCAAAGCCACTTGGCCACTGCGGGCTCTACTTCATCGCATTCCTTGCAA
AAGTATTACATCACGGGGGAGGCAGAGGGTTTCCCTGCCACGGTCTGA
Chromosome Location
6
Locus
6q25.1
External Identifiers
ResourceLink
UniProtKB IDP03372
UniProtKB Entry NameESR1_HUMAN
GenBank Protein ID31234
GenBank Gene IDX03635
GenAtlas IDESR1
HGNC IDHGNC:3467
General References
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Drug Relations

Drug Relations
DrugBank IDNameDrug groupPharmacological action?ActionsDetails
DB00255Diethylstilbestrolapproved, investigationalyesagonistDetails
DB00269Chlorotrianiseneinvestigational, withdrawnyesagonistDetails
DB00286Conjugated estrogensapprovedyesagonistDetails
DB00294Etonogestrelapproved, investigationalyesagonistDetails
DB00481Raloxifeneapproved, investigationalyesagonistDetails
DB00539Toremifeneapproved, investigationalyesmodulatorDetails
DB00655EstroneapprovedyesagonistDetails
DB00783Estradiolapproved, investigational, vet_approvedyesagonistDetails
DB00823Ethynodiol diacetateapprovedyesagonistDetails
DB00882Clomifeneapproved, investigationalyesantagonistagonistDetails
DB00890Dienestrolapproved, investigationalyesagonistDetails
DB00947Fulvestrantapproved, investigationalyesantagonistDetails
DB00977EthinylestradiolapprovedyesagonistDetails
DB00304DesogestrelapprovedyesagonistDetails
DB00367Levonorgestrelapproved, investigationalyesother/unknownDetails
DB00396Progesteroneapproved, vet_approvedunknownagonistinhibitordownregulatorDetails
DB00603Medroxyprogesterone acetateapproved, investigationalyesagonistDetails
DB00957Norgestimateapproved, investigationalyesagonistDetails
DB01185Fluoxymesteroneapproved, illicityesantagonistDetails
DB01196Estramustineapproved, investigationalyesagonistDetails
DB01406DanazolapprovedyesagonistDetails
DB01183Naloxoneapproved, vet_approvednoantagonistother/unknownDetails
DB02615Compound 19experimentalunknownDetails
DB02715Compound 18experimentalunknownDetails
DB03742Compound 4-DexperimentalunknownDetails
DB038021-[4-(Octahydro-Pyrido[1,2-a]Pyrazin-2-Yl)-Phenyl]-2-Phenyl-1,2,3,4-Tetrahydro-Isoquinolin-6-OlexperimentalunknownDetails
DB04468AfimoxifeneinvestigationalunknownDetails
DB044712-Phenyl-1-[4-(2-Piperidin-1-Yl-Ethoxy)-Phenyl]-1,2,3,4-Tetrahydro-Isoquinolin-6-OlexperimentalunknownDetails
DB04575QuinestrolapprovedyesagonistmodulatorDetails
DB00675TamoxifenapprovedyesantagonistagonistDetails
DB05233AP1081investigationalunknownDetails
DB04938Ospemifeneapproved, investigationalyesantagonistagonistDetails
DB01357MestranolapprovedyesagonistDetails
DB04573Estriolapproved, investigational, vet_approvedyesagonistDetails
DB05662NP-50301investigationalunknownDetails
DB05487CustirseninvestigationalunknownDetails
DB05882CHF 4227investigationalunknownDetails
DB05966TAS-108investigationalunknownDetails
DB06202Lasofoxifeneapproved, investigationalyesantagonistagonistnegative modulatorDetails
DB06249Arzoxifeneapproved, investigationalunknownDetails
DB06374ElacestrantinvestigationalunknownDetails
DB01065Melatoninapproved, nutraceutical, vet_approvedunknownantagonistDetails
DB0687117-METHYL-17-ALPHA-DIHYDROEQUILENINexperimentalunknownDetails
DB068984-(2-amino-1-methyl-1H-imidazo[4,5-b]pyridin-6-yl)phenolexperimentalunknownDetails
DB06927[5-HYDROXY-2-(4-HYDROXYPHENYL)-1-BENZOFURAN-7-YL]ACETONITRILEexperimentalunknownDetails
DB070864-[(1S,2S,5S)-5-(HYDROXYMETHYL)-8-METHYL-3-OXABICYCLO[3.3.1]NON-7-EN-2-YL]PHENOLexperimentalunknownDetails
DB070874-[(1S,2S,5S,9R)-5-(HYDROXYMETHYL)-8,9-DIMETHYL-3-OXABICYCLO[3.3.1]NON-7-EN-2-YL]PHENOLexperimentalunknownDetails
DB071954-[(1S,2S,5S)-5-(HYDROXYMETHYL)-6,8,9-TRIMETHYL-3-OXABICYCLO[3.3.1]NON-7-EN-2-YL]PHENOLexperimentalunknownDetails
DB07567(2R,3R,4S)-3-(4-HYDROXYPHENYL)-4-METHYL-2-[4-(2-PYRROLIDIN-1-YLETHOXY)PHENYL]CHROMAN-6-OLexperimentalunknownDetails
DB07638(3AS,4R,9BR)-2,2-DIFLUORO-4-(4-HYDROXYPHENYL)-1,2,3,3A,4,9B-HEXAHYDROCYCLOPENTA[C]CHROMEN-8-OLexperimentalunknownDetails
DB07678(9ALPHA,13BETA,17BETA)-2-[(1Z)-BUT-1-EN-1-YL]ESTRA-1,3,5(10)-TRIENE-3,17-DIOLexperimentalunknownDetails
DB07707(9BETA,11ALPHA,13ALPHA,14BETA,17ALPHA)-11-(METHOXYMETHYL)ESTRA-1(10),2,4-TRIENE-3,17-DIOLexperimentalunknownDetails
DB077083-CHLORO-2-(4-HYDROXYPHENYL)-2H-INDAZOL-5-OLexperimentalunknownDetails
DB077123-ETHYL-2-(4-HYDROXYPHENYL)-2H-INDAZOL-5-OLexperimentalunknownDetails
DB01645GenisteininvestigationalunknownDetails
DB07932dimethyl (1R,4S)-5,6-bis(4-hydroxyphenyl)-7-oxabicyclo[2.2.1]hepta-2,5-diene-2,3-dicarboxylateexperimentalunknownDetails
DB07933Erteberelexperimental, investigationalunknownDetails
DB07991N-[(1R)-3-(4-HYDROXYPHENYL)-1-METHYLPROPYL]-2-(2-PHENYL-1H-INDOL-3-YL)ACETAMIDEexperimentalunknownDetails
DB08020(3AS,4R,9BR)-4-(4-HYDROXYPHENYL)-6-(METHOXYMETHYL)-1,2,3,3A,4,9B-HEXAHYDROCYCLOPENTA[C]CHROMEN-8-OLexperimentalunknownDetails
DB080474-[1-allyl-7-(trifluoromethyl)-1H-indazol-3-yl]benzene-1,3-diolexperimentalunknownDetails
DB080484-(6-HYDROXY-1H-INDAZOL-3-YL)BENZENE-1,3-DIOLexperimentalunknownDetails
DB08320DIETHYL (1R,2S,3R,4S)-5,6-BIS(4-HYDROXYPHENYL)-7-OXABICYCLO[2.2.1]HEPT-5-ENE-2,3-DICARBOXYLATEexperimentalunknownDetails
DB083982-Amino-1-methyl-6-phenylimidazo(4,5-b)pyridineinvestigationalunknownDetails
DB085954-[(1S,2R,5S)-4,4,8-TRIMETHYL-3-OXABICYCLO[3.3.1]NON-7-EN-2-YL]PHENOLexperimentalunknownDetails
DB08737(3AS,4R,9BR)-4-(4-HYDROXYPHENYL)-1,2,3,3A,4,9B-HEXAHYDROCYCLOPENTA[C]CHROMEN-9-OLexperimentalunknownDetails
DB08773RALOXIFENE COREexperimentalunknownDetails
DB01108Trilostaneapproved, investigational, vet_approved, withdrawnyesallosteric modulatorDetails
DB01431AllylestrenolexperimentalunknownagonistDetails
DB04574Estrone sulfateapprovedyesagonistDetails
DB01708Prasteroneapproved, investigational, nutraceuticalunknownbinderDetails
DB06401Bazedoxifeneapproved, investigationalyesantagonistagonistDetails
DB09317Synthetic Conjugated Estrogens, AapprovedyesligandDetails
DB09318Synthetic Conjugated Estrogens, BapprovedyesligandDetails
DB09070Tiboloneapproved, investigationalyesantagonistagonistDetails
DB03467NaringeninexperimentalunknownDetails
DB06732beta-NaphthoflavoneexperimentalunknownDetails
DB04216Quercetinexperimental, investigationalunknownDetails
DB09086EugenolapprovedunknownDetails
DB02901Stanoloneillicit, investigationalunknownDetails
DB00624Testosteroneapproved, investigationalunknowninhibitorDetails
DB00648MitotaneapprovedunknownDetails
DB02746Phthalic AcidexperimentalunknownDetails
DB00431Lindaneapproved, withdrawnunknownDetails
DB01593Zincapproved, investigationalunknowncofactorDetails
DB00756Hexachloropheneapproved, withdrawnunknownDetails
DB01878BenzophenoneexperimentalunknownDetails
DB09535Octocryleneapproved, investigationalunknownDetails
DB01428Oxybenzoneapproved, investigationalunknownDetails
DB11219EnzacameneapprovedunknownDetails
DB04930Permethrinapproved, investigationalunknownDetails
DB02757PyrazoleexperimentalunknownDetails
DB07931HexestrolwithdrawnunknownDetails
DB12450Propyl GallateinvestigationalunknownDetails
DB02709Resveratrolapproved, experimental, investigationalunknownDetails
DB11478Zeranolexperimental, vet_approvedunknownDetails
DB09371NorethynodrelapprovedunknownDetails
DB02187EquilinexperimentalunknownDetails
DB11064Homosalateapproved, investigationalunknownDetails
DB00841DobutamineapprovedunknownDetails
DB11541Ractopaminevet_approvedunknownDetails
DB06710MethyltestosteroneapprovedunknownDetails
DB04824Phenolphthaleinapproved, withdrawnunknownagonistDetails
DB138692-Methoxy-6-{(E)-[(4-methylphenyl)imino]methyl}phenolexperimentalunknownDetails
DB13943Testosterone cypionateapprovedunknownDetails
DB13944Testosterone enanthateapprovedunknownDetails
DB13946Testosterone undecanoateapproved, investigationalunknownDetails
DB13951Stanolone acetateexperimentalunknownDetails
DB13952Estradiol acetateapproved, investigational, vet_approvedyesagonistDetails
DB13953Estradiol benzoateapproved, investigational, vet_approvedyesagonistDetails
DB13954Estradiol cypionateapproved, investigational, vet_approvedyesagonistDetails
DB13955Estradiol dienanthateapproved, investigational, vet_approvedyesagonistDetails
DB13956Estradiol valerateapproved, investigational, vet_approvedyesagonistDetails
DB09369Polyestradiol phosphateapprovedyesagonistDetails
DB11619GestrinoneapprovedunknownantagonistagonistDetails
DB14487Zinc acetateapproved, investigationalunknownDetails
DB14533Zinc chlorideapproved, investigationalunknownDetails
DB14641Estriol tripropionateexperimentalyesDetails