ESR1
Available structures PDB Ortholog search: PDBe RCSB List of PDB id codes 1A52, 1ERE, 1ERR, 1G50, 1GWQ, 1GWR, 1HCP, 1HCQ, 1L2I, 1PCG, 1QKT, 1QKU, 1R5K, 1SJ0, 1UOM, 1X7E, 1X7R, 1XP1, 1XP6, 1XP9, 1XPC, 1XQC, 1YIM, 1YIN, 1ZKY, 2AYR, 2B1V, 2B1Z, 2B23, 2BJ4, 2FAI, 2G44, 2G5O, 2I0J, 2IOG, 2IOK, 2JF9, 2JFA, 2LLO, 2LLQ, 2OCF, 2OUZ, 2P15, 2POG, 2Q6J, 2Q70, 2QA6, 2QA8, 2QAB, 2QE4, 2QGT, 2QGW, 2QH6, 2QR9, 2QSE, 2QXM, 2QXS, 2QZO, 2R6W, 2R6Y, 2YAT, 2YJA, 3CBM, 3CBO, 3CBP, 3DT3, 3ERD, 3ERT, 3HLV, 3HM1, 3L03, 3OS8, 3OS9, 3OSA, 3Q95, 3Q97, 3UU7, 3UUA, 3UUC, 3UUD, 4AA6, 4DMA, 4IU7, 4IUI, 4IV2, 4IV4, 4IVW, 4IVY, 4IW6, 4IW8, 4IWC, 4IWF, 4JC3, 4JDD, 4MG5, 4MG6, 4MG7, 4MG8, 4MG9, 4MGA, 4MGB, 4MGC, 4MGD, 4O6F, 4PP6, 4PPP, 4PPS, 4PXM, 4Q13, 4Q50, 4TUZ, 4TV1, 5AK2, 5AAV, 5ACC, 5AAU, 4XI3, 4ZN9, 5FQS, 5FQR, 5FQP, 5FQT, 5FQV, 4ZN7, 5E0W, 5DUG, 4ZUC, 5DXK, 5E19, 5DXQ, 5EI1, 5DXR, 5DVS, 5DZ1, 5E0X, 5DKB, 5DWI, 5E14, 5DXB, 5BPR, 5EIT, 5E15, 4ZNS, 5EGV, 5DL4, 5DWE, 4ZNT, 5EHJ, 5DYD, 5DWG, 4ZNV, 5DWJ, 5DID, 4ZUB, 5BNU, 5DMC, 5DK9, 5DIG, 5DUH, 5DKS, 5DMF, 5DU5, 5DY8, 4ZWH, 5DVV, 5DLR, 4ZWK, 5DRM, 5DP0, 5DKE, 5DZI, 5DZ3, 4ZNU, 5DIE, 5DZ0, 5E1C, 5HYR, 5BQ4, 4ZNW, 5DUE, 5DTV, 5DRJ, 5DKG, 4ZNH, 5BP6, 5DXG, 5DI7, 5DX3, 5DYB, 5DXP, 5DZH, 5DXM
Identifiers
Aliases	ESR1, ER, ESR, ESRA, ESTRR, Era, NR3A1, estrogen receptor 1
External IDs	OMIM: 133430; MGI: 1352467; HomoloGene: 47906; GeneCards: ESR1; OMA:ESR1 - orthologs
Gene location (Human) Chr. Chromosome 6 (human)[1] Band 6q25.1-q25.2 Start 151,656,691 bp[1] End 152,129,619 bp[1]
Gene location (Mouse) Chr. Chromosome 10 (mouse)[2] Band 10 A1|10 2.03 cM Start 4,561,593 bp[2] End 4,955,614 bp[2]
RNA expression pattern Bgee Human Mouse (ortholog) Top expressed in cervix epithelium vulva endometrium canal of the cervix right uterine tube ectocervix epithelium of lactiferous gland lactiferous duct body of uterus vagina Top expressed in gastrula vas deferens efferent ductule uterus decidua intercostal muscle triceps brachii muscle sternocleidomastoid muscle lumbar spinal ganglion temporal muscle More reference expression data BioGPS n/a
Gene ontology Molecular function DNA-binding transcription factor activity DNA-binding transcription activator activity, RNA polymerase II-specific nitric-oxide synthase regulator activity nuclear receptor activity estrogen response element binding transcription factor binding metal ion binding RNA polymerase II cis-regulatory region sequence-specific DNA binding steroid hormone receptor activity steroid binding beta-catenin binding zinc ion binding chromatin binding protein binding DNA binding sequence-specific DNA binding ATPase binding identical protein binding lipid binding core promoter sequence-specific DNA binding enzyme binding protein kinase binding TFIIB-class transcription factor binding TBP-class protein binding estrogen receptor activity estrogen receptor binding transcription coactivator binding phosphatidylinositol-4,5-bisphosphate 3-kinase activity DNA-binding transcription factor activity, RNA polymerase II-specific Cellular component cytoplasm membrane nucleus integral component of membrane Golgi apparatus plasma membrane nucleoplasm transcription preinitiation complex cytosol protein-containing complex Biological process epithelial cell development positive regulation of phospholipase C activity mammary gland alveolus development transcription by RNA polymerase II phospholipase C-activating G protein-coupled receptor signaling pathway epithelial cell proliferation involved in mammary gland duct elongation prostate epithelial cord arborization involved in prostate glandular acinus morphogenesis protein localization to chromatin steroid hormone mediated signaling pathway regulation of apoptotic process chromatin remodeling regulation of transcription, DNA-templated androgen metabolic process positive regulation of fibroblast proliferation mammary gland branching involved in pregnancy negative regulation of gene expression transcription, DNA-templated negative regulation of DNA-binding transcription factor activity cellular response to estrogen stimulus positive regulation of transcription, DNA-templated positive regulation of nitric-oxide synthase activity transcription initiation from RNA polymerase II promoter regulation of branching involved in prostate gland morphogenesis male gonad development positive regulation of DNA-binding transcription factor activity negative regulation of transcription by RNA polymerase II negative regulation of I-kappaB kinase/NF-kappaB signaling negative regulation of production of miRNAs involved in gene silencing by miRNA response to estrogen uterus development prostate epithelial cord elongation antral ovarian follicle growth vagina development positive regulation of cytosolic calcium ion concentration positive regulation of nitric oxide biosynthetic process signal transduction positive regulation of transcription by RNA polymerase II intracellular steroid hormone receptor signaling pathway regulation of inflammatory response response to estradiol regulation of toll-like receptor signaling pathway regulation of transcription by RNA polymerase II protein deubiquitination cellular response to estradiol stimulus intracellular estrogen receptor signaling pathway positive regulation of RNA polymerase II transcription preinitiation complex assembly stem cell differentiation regulation of Wnt signaling pathway regulation of intracellular estrogen receptor signaling pathway phosphatidylinositol phosphate biosynthetic process positive regulation of protein kinase B signaling Sources:Amigo / QuickGO
Orthologs Species Human Mouse Entrez 2099 13982 Ensembl ENSG00000091831 ENSMUSG00000019768 UniProt P03372 P19785 RefSeq (mRNA) NM_000125 NM_001122740 NM_001122741 NM_001122742 NM_001291230 NM_001291241 NM_001328100 NM_001385568 NM_001385569 NM_001385570 NM_001385571 NM_001385572 NM_007956 NM_001302531 NM_001302532 NM_001302533 RefSeq (protein) NP_000116 NP_001116212 NP_001116213 NP_001116214 NP_001278159 NP_001278170 NP_001315029 NP_001289460 NP_001289461 NP_001289462 NP_031982 Location (UCSC) Chr 6: 151.66 – 152.13 Mb Chr 10: 4.56 – 4.96 Mb PubMed search [3] [4]
Wikidata
View/Edit Human View/Edit Mouse

Estrogen receptor alpha (ERα), also known as NR3A1 (nuclear receptor subfamily 3, group A, member 1), is one of two main types of estrogen receptor, a nuclear receptor (mainly found as a chromatin-binding protein^[5]) that is activated by the sex hormone estrogen. In humans, ERα is encoded by the gene ESR1 (EStrogen Receptor 1).^[6][7][8]

Structure

The estrogen receptor (ER) is a ligand-activated transcription factor composed of several domains important for hormone binding, DNA binding, and activation of transcription.^[9] Alternative splicing results in several ESR1 mRNA transcripts, which differ primarily in their 5-prime untranslated regions. The translated receptors show less variability.^[10][11]

Ligands

Agonists

Non-selective

• Endogenous estrogens (e.g., estradiol, estrone, estriol, estetrol)
• Natural estrogens (e.g., conjugated equine estrogens)
• Synthetic estrogens (e.g., ethinylestradiol, diethylstilbestrol)

Selective

Agonists of ERα selective over ERβ include:

• Propylpyrazoletriol (PPT)
• 16α-LE₂ (Cpd1471)
• 16α-IE₂
• ERA-63 (ORG-37663)
• SKF-82,958 – also a D₁-like receptor full agonist
• (R,R)-Tetrahydrochrysene ((R,R)-THC) – actually not selective over ERβ, but rather an antagonist instead of an agonist of ERβ

Mixed

• Phytoestrogens (e.g., coumestrol, daidzein, genistein, miroestrol)
• Selective estrogen receptor modulators (e.g., tamoxifen, clomifene, raloxifene)

Antagonists

Non-selective

• Antiestrogens (e.g., fulvestrant, ICI-164384, ethamoxytriphetol)

Selective

Antagonists of ERα selective over ERβ include:

• Methylpiperidinopyrazole (MPP)

Affinities

Zdroj:https://en.wikipedia.org?pojem=Estrogen_receptor_alpha
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Affinities of estrogen receptor ligands for the ERα and ERβ

Ligand	Other names	Relative binding affinities (RBA, %)a		Absolute binding affinities (Ki, nM)a		Action
		ERα	ERβ	ERα	ERβ
Estradiol	E2; 17β-Estradiol	100	100	0.115 (0.04–0.24)	0.15 (0.10–2.08)	Estrogen
Estrone	E1; 17-Ketoestradiol	16.39 (0.7–60)	6.5 (1.36–52)	0.445 (0.3–1.01)	1.75 (0.35–9.24)	Estrogen
Estriol	E3; 16α-OH-17β-E2	12.65 (4.03–56)	26 (14.0–44.6)	0.45 (0.35–1.4)	0.7 (0.63–0.7)	Estrogen
Estetrol	E4; 15α,16α-Di-OH-17β-E2	4.0	3.0	4.9	19	Estrogen
Alfatradiol	17α-Estradiol	20.5 (7–80.1)	8.195 (2–42)	0.2–0.52	0.43–1.2	Metabolite
16-Epiestriol	16β-Hydroxy-17β-estradiol	7.795 (4.94–63)	50	?	?	Metabolite
17-Epiestriol	16α-Hydroxy-17α-estradiol	55.45 (29–103)	79–80	?	?	Metabolite
16,17-Epiestriol	16β-Hydroxy-17α-estradiol	1.0	13	?	?	Metabolite
2-Hydroxyestradiol	2-OH-E2	22 (7–81)	11–35	2.5	1.3	Metabolite
2-Methoxyestradiol	2-MeO-E2	0.0027–2.0	1.0	?	?	Metabolite
4-Hydroxyestradiol	4-OH-E2	13 (8–70)	7–56	1.0	1.9	Metabolite
4-Methoxyestradiol	4-MeO-E2	2.0	1.0	?	?	Metabolite
2-Hydroxyestrone	2-OH-E1	2.0–4.0	0.2–0.4	?	?	Metabolite
2-Methoxyestrone	2-MeO-E1	<0.001–<1	<1	?	?	Metabolite
4-Hydroxyestrone	4-OH-E1	1.0–2.0	1.0	?	?	Metabolite
4-Methoxyestrone	4-MeO-E1	<1	<1	?	?	Metabolite
16α-Hydroxyestrone	16α-OH-E1; 17-Ketoestriol	2.0–6.5	35	?	?	Metabolite
2-Hydroxyestriol	2-OH-E3	2.0	1.0	?	?	Metabolite
4-Methoxyestriol	4-MeO-E3	1.0	1.0	?	?	Metabolite
Estradiol sulfate	E2S; Estradiol 3-sulfate	<1	<1	?	?	Metabolite
Estradiol disulfate	Estradiol 3,17β-disulfate	0.0004	?	?	?	Metabolite
Estradiol 3-glucuronide	E2-3G	0.0079	?	?	?	Metabolite
Estradiol 17β-glucuronide	E2-17G	0.0015	?	?	?	Metabolite
Estradiol 3-gluc. 17β-sulfate	E2-3G-17S	0.0001	?	?	?	Metabolite
Estrone sulfate	E1S; Estrone 3-sulfate	<1	<1	>10	>10	Metabolite
Estradiol benzoate	EB; Estradiol 3-benzoate	10	?	?	?	Estrogen
Estradiol 17β-benzoate	E2-17B	11.3	32.6	?	?	Estrogen
Estrone methyl ether	Estrone 3-methyl ether	0.145	?	?	?	Estrogen
ent-Estradiol	1-Estradiol	1.31–12.34	9.44–80.07	?	?	Estrogen
Equilin	7-Dehydroestrone	13 (4.0–28.9)	13.0–49	0.79	0.36	Estrogen
Equilenin	6,8-Didehydroestrone	2.0–15	7.0–20	0.64	0.62	Estrogen
17β-Dihydroequilin	7-Dehydro-17β-estradiol	7.9–113	7.9–108	0.09	0.17	Estrogen
17α-Dihydroequilin	7-Dehydro-17α-estradiol	18.6 (18–41)	14–32	0.24	0.57	Estrogen
17β-Dihydroequilenin	6,8-Didehydro-17β-estradiol	35–68	90–100	0.15	0.20	Estrogen
17α-Dihydroequilenin	6,8-Didehydro-17α-estradiol	20	49	0.50	0.37	Estrogen
Δ8-Estradiol	8,9-Dehydro-17β-estradiol	68	72	0.15	0.25	Estrogen
Δ8-Estrone	8,9-Dehydroestrone	19	32	0.52	0.57	Estrogen
Ethinylestradiol	EE; 17α-Ethynyl-17β-E2	120.9 (68.8–480)	44.4 (2.0–144)	0.02–0.05	0.29–0.81	Estrogen
Mestranol	EE 3-methyl ether	?	2.5	?	?	Estrogen
Moxestrol	RU-2858; 11β-Methoxy-EE	35–43	5–20	0.5	2.6	Estrogen
Methylestradiol	17α-Methyl-17β-estradiol	70	44	?	?	Estrogen
Diethylstilbestrol	DES; Stilbestrol	129.5 (89.1–468)	219.63 (61.2–295)	0.04	0.05	Estrogen
Hexestrol	Dihydrodiethylstilbestrol	153.6 (31–302)	60–234	0.06	0.06	Estrogen
Dienestrol	Dehydrostilbestrol	37 (20.4–223)	56–404	0.05	0.03	Estrogen
Benzestrol (B2)	–	114	?	?	?	Estrogen
Chlorotrianisene	TACE	1.74	?	15.30	?	Estrogen
Triphenylethylene	TPE	0.074	?	?	?	Estrogen
Triphenylbromoethylene	TPBE	2.69	?	?	?	Estrogen
Tamoxifen	ICI-46,474	3 (0.1–47)	3.33 (0.28–6)	3.4–9.69	2.5	SERM
Afimoxifene	4-Hydroxytamoxifen; 4-OHT	100.1 (1.7–257)	10 (0.98–339)	2.3 (0.1–3.61)	0.04–4.8	SERM
Toremifene	4-Chlorotamoxifen; 4-CT	?	?	7.14–20.3	15.4	SERM
Clomifene	MRL-41	25 (19.2–37.2)	12	0.9	1.2	SERM
Cyclofenil	F-6066; Sexovid	151–152	243	?	?	SERM
Nafoxidine	U-11,000A	30.9–44