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
- FunctionsATPase 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 bindingProcessesandrogen 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 developmentComponentscytoplasm / 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
Resource Link UniProtKB ID P03372 UniProtKB Entry Name ESR1_HUMAN GenBank Protein ID 31234 GenBank Gene ID X03635 GenAtlas ID ESR1 HGNC ID HGNC:3467 - General References
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Drug Relations
- Drug Relations
DrugBank ID Name Drug group Pharmacological action? Actions Details DB00255 Diethylstilbestrol approved, investigational, withdrawn yes agonist Details DB00269 Chlorotrianisene investigational, withdrawn yes agonist Details DB00286 Conjugated estrogens approved yes agonist Details DB00481 Raloxifene approved, investigational yes agonist Details DB00539 Toremifene approved, investigational yes modulator Details DB00655 Estrone approved yes agonist Details DB00783 Estradiol approved, investigational, vet_approved yes agonist Details DB00823 Ethynodiol diacetate approved yes agonist Details DB00882 Clomifene approved, investigational yes antagonistagonist Details DB00890 Dienestrol approved, investigational yes agonist Details DB00947 Fulvestrant approved, investigational yes antagonist Details DB00977 Ethinylestradiol approved yes agonist Details DB00304 Desogestrel approved yes agonist Details DB00367 Levonorgestrel approved, investigational yes other/unknown Details DB00396 Progesterone approved, vet_approved unknown agonistinhibitordownregulator Details DB00603 Medroxyprogesterone acetate approved, investigational yes agonist Details DB00957 Norgestimate approved, investigational yes agonist Details DB01185 Fluoxymesterone approved, illicit yes antagonist Details DB01196 Estramustine approved, investigational yes agonist Details DB01406 Danazol approved yes agonist Details DB01183 Naloxone approved, vet_approved no antagonistother/unknown Details DB02615 Compound 19 experimental unknown Details DB02715 Compound 18 experimental unknown Details DB03742 Compound 4-D experimental unknown Details DB03802 1-[4-(Octahydro-Pyrido[1,2-a]Pyrazin-2-Yl)-Phenyl]-2-Phenyl-1,2,3,4-Tetrahydro-Isoquinolin-6-Ol experimental unknown Details DB04468 Afimoxifene investigational unknown Details DB04471 2-Phenyl-1-[4-(2-Piperidin-1-Yl-Ethoxy)-Phenyl]-1,2,3,4-Tetrahydro-Isoquinolin-6-Ol experimental unknown Details DB04575 Quinestrol approved yes agonistmodulator Details DB00675 Tamoxifen approved yes antagonistagonist Details DB05233 AP1081 investigational unknown Details DB04938 Ospemifene approved, investigational yes antagonistagonist Details DB01357 Mestranol approved yes agonist Details DB04573 Estriol approved, investigational, vet_approved yes agonist Details DB05662 NP-50301 investigational unknown Details DB05487 Custirsen investigational unknown Details DB05882 CHF 4227 investigational unknown Details DB05966 TAS-108 investigational unknown Details DB06202 Lasofoxifene approved, investigational yes antagonistagonistnegative modulator Details DB06249 Arzoxifene approved, investigational unknown Details DB06374 Elacestrant approved, investigational unknown antagonist Details DB01065 Melatonin approved, nutraceutical, vet_approved unknown antagonist Details DB06871 17-METHYL-17-ALPHA-DIHYDROEQUILENIN experimental unknown Details DB06898 4-(2-amino-1-methyl-1H-imidazo[4,5-b]pyridin-6-yl)phenol experimental unknown Details DB06927 [5-HYDROXY-2-(4-HYDROXYPHENYL)-1-BENZOFURAN-7-YL]ACETONITRILE experimental unknown Details DB07086 4-[(1S,2S,5S)-5-(HYDROXYMETHYL)-8-METHYL-3-OXABICYCLO[3.3.1]NON-7-EN-2-YL]PHENOL experimental unknown Details DB07087 4-[(1S,2S,5S,9R)-5-(HYDROXYMETHYL)-8,9-DIMETHYL-3-OXABICYCLO[3.3.1]NON-7-EN-2-YL]PHENOL experimental unknown Details DB07195 4-[(1S,2S,5S)-5-(HYDROXYMETHYL)-6,8,9-TRIMETHYL-3-OXABICYCLO[3.3.1]NON-7-EN-2-YL]PHENOL experimental unknown Details DB07567 (2R,3R,4S)-3-(4-HYDROXYPHENYL)-4-METHYL-2-[4-(2-PYRROLIDIN-1-YLETHOXY)PHENYL]CHROMAN-6-OL experimental unknown Details DB07638 (3AS,4R,9BR)-2,2-DIFLUORO-4-(4-HYDROXYPHENYL)-1,2,3,3A,4,9B-HEXAHYDROCYCLOPENTA[C]CHROMEN-8-OL experimental unknown Details DB07678 (9ALPHA,13BETA,17BETA)-2-[(1Z)-BUT-1-EN-1-YL]ESTRA-1,3,5(10)-TRIENE-3,17-DIOL experimental unknown Details DB07707 (9BETA,11ALPHA,13ALPHA,14BETA,17ALPHA)-11-(METHOXYMETHYL)ESTRA-1(10),2,4-TRIENE-3,17-DIOL experimental unknown Details DB07708 3-CHLORO-2-(4-HYDROXYPHENYL)-2H-INDAZOL-5-OL experimental unknown Details DB07712 3-ETHYL-2-(4-HYDROXYPHENYL)-2H-INDAZOL-5-OL experimental unknown Details DB01645 Genistein investigational unknown Details DB07932 dimethyl (1R,4S)-5,6-bis(4-hydroxyphenyl)-7-oxabicyclo[2.2.1]hepta-2,5-diene-2,3-dicarboxylate experimental unknown Details DB07933 Erteberel experimental, investigational unknown Details DB07991 N-[(1R)-3-(4-HYDROXYPHENYL)-1-METHYLPROPYL]-2-(2-PHENYL-1H-INDOL-3-YL)ACETAMIDE experimental unknown Details DB08020 (3AS,4R,9BR)-4-(4-HYDROXYPHENYL)-6-(METHOXYMETHYL)-1,2,3,3A,4,9B-HEXAHYDROCYCLOPENTA[C]CHROMEN-8-OL experimental unknown Details DB08047 4-[1-allyl-7-(trifluoromethyl)-1H-indazol-3-yl]benzene-1,3-diol experimental unknown Details DB08048 4-(6-HYDROXY-1H-INDAZOL-3-YL)BENZENE-1,3-DIOL experimental unknown Details DB08320 DIETHYL (1R,2S,3R,4S)-5,6-BIS(4-HYDROXYPHENYL)-7-OXABICYCLO[2.2.1]HEPT-5-ENE-2,3-DICARBOXYLATE experimental unknown Details DB08398 2-Amino-1-methyl-6-phenylimidazo(4,5-b)pyridine investigational unknown Details DB08595 4-[(1S,2R,5S)-4,4,8-TRIMETHYL-3-OXABICYCLO[3.3.1]NON-7-EN-2-YL]PHENOL experimental unknown Details DB08737 (3AS,4R,9BR)-4-(4-HYDROXYPHENYL)-1,2,3,3A,4,9B-HEXAHYDROCYCLOPENTA[C]CHROMEN-9-OL experimental unknown Details DB08773 2-(4-hydroxyphenyl)benzo[b]thiophen-6-ol experimental unknown Details DB01108 Trilostane approved, investigational, vet_approved, withdrawn yes allosteric modulator Details DB01431 Allylestrenol experimental unknown agonist Details DB04574 Estrone sulfate approved yes agonist Details DB01708 Prasterone approved, investigational, nutraceutical unknown binder Details DB06401 Bazedoxifene approved, investigational yes antagonistagonist Details DB09317 Synthetic Conjugated Estrogens, A approved yes ligand Details DB09318 Synthetic Conjugated Estrogens, B approved yes ligand Details DB09070 Tibolone approved, investigational yes antagonistagonist Details DB03467 Naringenin experimental unknown Details DB06732 beta-Naphthoflavone experimental unknown Details DB04216 Quercetin experimental, investigational unknown Details DB09086 Eugenol approved unknown Details DB02901 Stanolone illicit, investigational unknown Details DB00624 Testosterone approved, investigational unknown inhibitor Details DB00648 Mitotane approved unknown Details DB02746 Phthalic Acid experimental unknown Details DB00431 Lindane approved, withdrawn unknown Details DB01593 Zinc approved, investigational unknown cofactor Details DB00756 Hexachlorophene approved, withdrawn unknown Details DB01878 Benzophenone experimental unknown Details DB09535 Octocrylene approved, investigational unknown Details DB01428 Oxybenzone approved, investigational unknown Details DB11219 Enzacamene approved unknown Details DB04930 Permethrin approved, investigational unknown Details DB02757 Pyrazole experimental unknown Details DB07931 Hexestrol withdrawn unknown Details DB12450 Propyl Gallate investigational unknown Details DB02709 Resveratrol investigational unknown Details DB11478 Zeranol experimental, vet_approved unknown Details DB09371 Norethynodrel approved unknown Details DB02187 Equilin experimental unknown Details DB11064 Homosalate approved, investigational unknown Details DB00841 Dobutamine approved unknown Details DB11541 Ractopamine vet_approved unknown Details DB06710 Methyltestosterone approved unknown Details DB04824 Phenolphthalein approved, withdrawn unknown agonist Details DB13869 2-Methoxy-6-{(E)-[(4-methylphenyl)imino]methyl}phenol experimental unknown Details DB13943 Testosterone cypionate approved unknown Details DB13944 Testosterone enanthate approved unknown Details DB13951 Stanolone acetate experimental unknown Details DB13952 Estradiol acetate approved, investigational, vet_approved yes agonist Details DB13953 Estradiol benzoate approved, investigational, vet_approved yes agonist Details DB13954 Estradiol cypionate approved, investigational, vet_approved yes agonist Details DB13955 Estradiol dienanthate approved, investigational, vet_approved yes agonist Details DB13956 Estradiol valerate approved, investigational, vet_approved yes agonist Details DB09369 Polyestradiol phosphate approved yes agonist Details DB11619 Gestrinone approved unknown antagonistagonist Details DB14487 Zinc acetate approved, investigational unknown Details DB14533 Zinc chloride approved, investigational unknown binder Details DB14641 Estriol tripropionate experimental yes Details DB14548 Zinc sulfate, unspecified form approved, experimental unknown binder Details DB15690 Fluoroestradiol F-18 approved unknown binder Details DB12235 Estetrol approved, investigational unknown agonistmodulatorregulator Details DB13310 Ormeloxifene experimental unknown modulator Details DB00421 Spironolactone approved unknown agonist Details