Product Details

Purity

Greater than 90% as determined by SDS-PAGE.

Target Names

ESR1

Uniprot No.

P03372

Research Area

Transcription

Alternative Names

7*/654 isoform; 7*/819 2 isoform; 7*/822 isoform; 8*/901 isoform; 8*/941 isoform; DKFZp686N23123; ER alpha; ER; ER-alpha; Era; ESR; ESR1; ESR1_HUMAN; ESRA; Estradiol receptor; Estrogen nuclear receptor alpha; Estrogen receptor 1; Estrogen receptor alpha 3*,4,5,6,7*/822 isoform; Estrogen receptor alpha; Estrogen receptor alpha delta 3*,4,5,6,7*,8*/941 isoform; Estrogen receptor alpha delta 3*,4,5,6,7*/819 2 isoform; Estrogen receptor alpha delta 4 +49 isoform; Estrogen receptor alpha delta 4*,5,6,7*/654 isoform; Estrogen receptor alpha delta 4*,5,6,7,8*/901 isoform; Estrogen receptor alpha E1 E2 1 2; Estrogen receptor alpha E1 N2 E2 1 2; Estrogen receptor; ESTRR; NR3A1; Nuclear receptor subfamily 3 group A member 1

Species

Homo sapiens (Human)

Source

Yeast

Expression Region

10-595aa

Target Protein Sequence

SGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALLDAEPPILYSEYDPTRPFSEASMMGLLTNLADRELVHMINWAKRVPGFVDLTLHDQVHLLECAWLEILMIGLVWRSMEHPGKLLFAPNLLLDRNQGKCVEGMVEIFDMLLATSSRFRMMNLQGEEFVCLKSIILLNSGVYTFLSSTLKSLEEKDHIHRVLDKITDTLIHLMAKAGLTLQQQHQRLAQLLLILSHIRHMSNKGMEHLYSMKCKNVVPLYDLLLEMLDAHRLHAPTSRGGASVEETDQSHLATAGSTSSHSLQKYYITGEAEGFPATV
Note: The complete sequence including tag sequence, target protein sequence and linker sequence could be provided upon request.

Mol. Weight

67.2kDa

Protein Length

Partial

Tag Info

N-terminal 6xHis-tagged

Form

Liquid or Lyophilized powder
Note: We will preferentially ship the format that we have in stock, however, if you have any special requirement for the format, please remark your requirement when placing the order, we will prepare according to your demand.

Buffer

If the delivery form is liquid, the default storage buffer is Tris/PBS-based buffer, 5%-50% glycerol.
Note: If you have any special requirement for the glycerol content, please remark when you place the order.
If the delivery form is lyophilized powder, the buffer before lyophilization is Tris/PBS-based buffer, 6% Trehalose.

Reconstitution

We recommend that this vial be briefly centrifuged prior to opening to bring the contents to the bottom. Please reconstitute protein in deionized sterile water to a concentration of 0.1-1.0 mg/mL.We recommend to add 5-50% of glycerol (final concentration) and aliquot for long-term storage at -20°C/-80°C. Our default final concentration of glycerol is 50%. Customers could use it as reference.

Troubleshooting and FAQs

Protein FAQs

Storage Condition

Store at -20°C/-80°C upon receipt, aliquoting is necessary for mutiple use. Avoid repeated freeze-thaw cycles.

Shelf Life

The shelf life is related to many factors, storage state, buffer ingredients, storage temperature and the stability of the protein itself.
Generally, the shelf life of liquid form is 6 months at -20°C/-80°C. The shelf life of lyophilized form is 12 months at -20°C/-80°C.

Lead Time

3-7 business days

Notes

Repeated freezing and thawing is not recommended. Store working aliquots at 4°C for up to one week.

Datasheet & COA

Please contact us to get it.

Description

The expression vector recombined with the recombinant DNA was transfected into the yeast cells for expression. The recombinant DNA resulted from the fusion of the gene coding for the 10-595aa of the human ESR1 protein and the N-terminal 6xHis tag gene. The product was purified and isolated to get the recombinant human ESR1 protein with N-terminal 6xHis tag. The purity of this recombinant ESR1 protein reaches up to 90%. Under SDS-PAGE condition, this recombinant ESR1 protein showed a band with a molecular weight of about 50-90 kDa on the gel. It may be used in the studies of ESR1-involving transcription.

ESR1 is a gene encoding a protein named estrogen receptor (abbreviated ESR1) and belongs to nuclear hormone receptor family. The canonical protein consists of an N-terminal ligand-independent transactivation domain, a central DNA binding domain, a hinge domain and a C-terminal ligand-dependent transactivation domain. The protein localizes to the nucleus where it may form either a homodimer or a heterodimer with estrogen receptor 2. Diseases associated with ESR1 include Estrogen Resistance and breast cancer. ESR1 mutations and mRNA splice variants are likely to emerge during treatment and can therefore only be observed in tumor cells obtained during or after treatment.

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Target Background

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. Essential for MTA1-mediated transcriptional regulation of BRCA1 and BCAS3.; 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. Binds to ERE and inhibits isoform 1.

Gene References into Functions

Estrogen-induced miR-191 was identified as a direct upstream regulator of DAB2 in ER-positive breast cancer cells. PMID: 29247596
the whole-genome insights carried in this work can help fully understanding biological roles of ER1 in breast cancer. PMID: 30301189
there was a relationship between rs2046210 and rs3803662, and the risk of developing this disease in Vietnamese women. The A allele is the risk allele for both rs2046210 (OR [95% CI] = 1.43 [1.14 - 1.78], P = 0.0015) and rs3803662 (OR [95% CI] = 1.45 [1.16 - 1.83], P = 0.001). We conclude that two polymorphisms, rs2046210 in ESR1 and rs3803662 in TNRC9, are associated with breast cancer risk in the Vietnamese population. PMID: 30078824
that Oestrogen receptor alpha can enhance the odonto/osteogenic differentiation of stem cells from apical papilla via ERK and JNK MAPK pathways PMID: 30069950
No association between polymorphisms in genes encoding estrogen receptors (ESR1 and ESR2) and excreted BPA levels was found in orthodontic patients after bracket bonding. PMID: 29961922
Analysis of the genome-wide ER binding sites identified mutant ER unique recruitment mediating the allele-specific transcriptional program PMID: 29438694
study describes RNF8 as a co-activator of ERalpha increases ERalpha stability via post-transcriptional pathway, and provides a new insight into mechanisms for RNF8 to promote cell growth of ERalpha-positive breast cancer. PMID: 28216286
Reduced expression of ERbeta1 in female ERalpha-negative papillary thyroid carcinoma patients is associated with greater progression of the disease. PMID: 29655286
heterogeneous distribution in deep infiltrating endometriosis PMID: 29383962
ER-alpha36/EGFR signaling loop promotes growth of hepatocellular carcinoma cells PMID: 29481815
This study aimed to determine the presence and localization of oestrogen receptors (ERs), progesterone receptors (PRs), and androgen receptors (ARs) in both healthy and varicose vein wall cells and their relationship with gender. PMID: 30250632
Estrogen receptor-alpha was expressed only in women and showed a positive correlation with the amount of fungi in oral paracoccidioidomycosis, while progesterone receptor was observed in both genders and exhibited no correlation with estrogen receptor-alpha or fungi counting. PMID: 29796757
ERalpha upregulates vinculin expression in breast cancer cells; Loss of vinculin promotes amoeboid features of cancer cells PMID: 28266545
polymorphisms do not predict in vitro fertilization outcome PMID: 29916276
High ESR1 expression is associated with metastasis in breast Cancer. PMID: 29187405
The G/G XbaI genotype of ESR1 gene is associated with breast cancer risk. PMID: 29893332
miR-221 may impair the protective effect of estrogen in degenerated cartilaginous endplate cells through targeting estrogen receptor alpha PMID: 29529124
Results showed that NAT1 and ESR1 expression were increased in primary breast tumor samples compared with normal breast tissue samples, and in ER+ primary breast tumors compared with ER- tumors. Also, NAT1 and ESR1 expression seems to have overlapping regulation. PMID: 29901116
all the patients without these mutations by molecular barcode next-generation sequencing (MB-NGS) were found to have no mutations by ddPCR. In conclusion, MB-NGS could successfully detect ESR1 mutations in cfDNA with a higher sensitivity of 0.1% than conventional NGS and was considered as clinically useful as ddPCR PMID: 28905136
In summary, an association between the presence of the particular genotypes at the three ESR1 polymorphisms (rs2234693, rs6902771, rs7774230) and one ESR2 polymorphism (rs3020449), and the presence of metabolic syndrome in postmenopausal women was found. PMID: 30049354
higher frequency of ESR1 and PIK3CA mutations in the plasma than in the serum in 33 MBC patients; therefore, serum samples should not be considered the preferred source of cfDNA. PMID: 29689710
These results suggest that miR-125a-3p can function as a novel tumor suppressor in ER(+) breast cancer by targeting CDK3, which may be a potential therapeutic approach for TamR breast cancer therapy PMID: 28939591
A major finding of our study is that one out of five (20%) patients with breast cancer BM had a receptor discrepancy between the primary tumor and the subsequent BM, with loss of hormone receptors (ER and/or PR) expression, and gain of HER2 overexpression as the most commonly observed changes PMID: 28975433
Here the authors report a nodal role of IGF-IR in the regulation of ERalpha-positive breast cancer cell aggressiveness and the regulation of expression levels of several extracellular matrix molecules. PMID: 28079144
The associations between PvuII (T>C) and XbaI (A>G) polymorphisms of estrogen receptor alpha (ESR1) gene with type 2 diabetes mellitus (T2DM) or metabolic syndrome (MetS), are reported. PMID: 29883973
The ERalpha gene seems to play a key role in stress urinary incontinence in the premenopausal period. PMID: 29769420
Study reports the first discovery of naturally occurring ESR1 (Y537C) and ESR1 (Y537S) mutations in MCF7 and SUM44 ESR1-positive cell lines after acquisition of resistance to long-term-estrogen-deprivation (LTED) and subsequent resistance to fulvestrant (ICIR). Mutations were enriched with time, impacted on ESR1 binding to the genome and altered the ESR1 interactome. PMID: 29192207
Concomitant high expression of ERalpha36, GRP78 and GRP94 is associated with aggressive papillary thyroid cancer behavior and may be used as a predictor for extrathyroid extension, lymph node metastasis, and distant metastasis. PMID: 29368272
Estrogen receptor-1 is a key regulator of HIV-1 latency that imparts gender-specific restrictions on the latent reservoir. PMID: 30061382
Down-regulation of ESR1 gene expression was enhanced by the development of the breast cancer. PMID: 29543921
The aim of the present study was to assess whether fibrosis markers, estrogen receptor (ER)alpha and the stromal derived factor (SDF)1/CXC chemokine receptor type 4 (CXCR4) axis are abnormally expressed in Intrauterine adhesions endometrium. PMID: 29568895
The frequency of alleles and genotypes of polymorphisms FSHR(-29G/A) and ESRI (XbaI A/G) in women with normal to poor response did not have significant correlation. PMID: 29526845
Each estrogen receptor alpha and estrogen receptor beta gene polymorphism might have different impact on postmenopausal osteoporosis risk and bone mineral density in various ethnicities. PMID: 29458346
The results suggest that minor allele A of ESR1 gene is associated with the development of arterial hypertension in men. PMID: 29658078
Study found that tamoxifen treatment induced a decrease in PRMT2 and an increase in ER-alpha36 as well as ER-alpha36-mediated non-genomic effect in MDA-MB-231 breast cancer cell line. PMID: 29620287
ESR1 mutations are not associated with clinical resistance to fulvestrant in breast cancer patients. PMID: 27174596
verexpression of COPS5, through its isopeptidase activity, leads to ubiquitination and proteasome-mediated degradation of NCoR, a key corepressor for ERalpha and tamoxifen-mediated suppression of ERalpha target genes. PMID: 27375289
ESR alpha PvuII and XbaI polymorphisms have no association with ; systemic lupus erythematosus. The combination of the TC/AA and CC/GG genotypes were associated with SLE susceptibility. PMID: 29356461
Estrogen receptor (ER) and progesterone receptor (PR) expression in endometrial carcinoma (EC) were significantly higher than those in the paracarcinoma tissue and control. PMID: 29081408
ESR1 promoter methylation was an independent risk factor and had a high value to predict 28-day mortality from acute-on-chronic hepatitis B liver failure PMID: 29082740
by analyzing different estrogen receptor-alpha(ER-a)-positive and ER-a-negative breast cancer cell lines, we defined the role of CCN5 in the leptin-mediated regulation of growth and invasive capacity. PMID: 29370782
This study identified ESR1 as a direct target of miR-301a-3p. PMID: 29763890
Authors report for the first time the presence of ESR1 methylation in plasma ctDNA of patients with HGSC. The agreement between ESR1 methylation in primary tumors and paired ctDNA is statistically significant. PMID: 29807696
this study reports the development of a novel class of ERa AF2 inhibitors, which have the potential to effectively inhibit ERa activity by a unique mechanism and to circumvent the issue of mutation-driven resistance in breast cancer PMID: 29462880
the P2X7R rs3751143 and ER-alpha PvuII two-locus interaction confers a significantly high susceptibility to osteoporosis in Chinese postmenopausal women. PMID: 28884379
Alcohol consumption may have differential effects on concordant and discordant receptor subtypes of breast cancer. PMID: 29353824
ERalpha and ERbeta mRNA expression was significantly higher (p < 0.05) in tumour tissues relative to their paired normal mucosa and correlated inversely with survival outcome PMID: 29390981
High ESR1 expression is associated with Papillary Thyroid Carcinoma. PMID: 28124274
Oral administration of RAD140 substantially inhibited the growth of AR/ER(+) breast cancer patient-derived xenografts (PDX). Activation of AR and suppression of ER pathway, including the ESR1 gene, were seen with RAD140 treatment. PMID: 28974548
Polymorphism in the ERalpha gene is associated with an increased risk for advanced Pelvic Organ Prolapse. However, polymorphism in the LAMC1 gene does not seem to be associated with such risk. PMID: 29241914

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Involvement in disease

Estrogen resistance (ESTRR)

Subcellular Location

[Isoform 1]: Nucleus. Cytoplasm. Cell membrane; Peripheral membrane protein; Cytoplasmic side.; Nucleus. Golgi apparatus. Cell membrane. Note=Colocalizes with ZDHHC7 and ZDHHC21 in the Golgi apparatus where most probably palmitoylation occurs. Associated with the plasma membrane when palmitoylated.

Protein Families

Nuclear hormone receptor family, NR3 subfamily

Tissue Specificity

Widely expressed. Not expressed in the pituitary gland.; [Isoform 3]: Widely expressed, however not expressed in the pituitary gland.

Database Links

HGNC: 3467

OMIM: 133430

KEGG: hsa:2099

STRING: 9606.ENSP00000206249

UniGene: Hs.208124

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