| DTT Name |
HUMAN estrogen receptor (ESR1)
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| Synonyms |
Nuclear receptor subfamily 3 group A member 1; NR3A1; Estradiol receptor; ESR; ER-alpha; ER |
| Gene Name |
ESR1
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| BioChemical Class |
Nuclear hormone receptor
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| UniProt ID |
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| TTD ID |
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| 3D Structure |
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| Sequence |
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAY
EFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPF
LQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAK
ETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQAC
RLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKR
SKKNSLALSLTADQMVSALLDAEPPILYSEYDPTRPFSEASMMGLLTNLADRELVHMINW
AKRVPGFVDLTLHDQVHLLECAWLEILMIGLVWRSMEHPGKLLFAPNLLLDRNQGKCVEG
MVEIFDMLLATSSRFRMMNLQGEEFVCLKSIILLNSGVYTFLSSTLKSLEEKDHIHRVLD
KITDTLIHLMAKAGLTLQQQHQRLAQLLLILSHIRHMSNKGMEHLYSMKCKNVVPLYDLL
LEMLDAHRLHAPTSRGGASVEETDQSHLATAGSTSSHSLQKYYITGEAEGFPATV
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| 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.
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| KEGG Pathway |
- Endocrine resistance (hsa01522 )
- Estrogen signaling pathway (hsa04915 )
- Prolactin signaling pathway (hsa04917 )
- Thyroid hormone signaling pathway (hsa04919 )
- Endocrine and other factor-regulated calcium reabsorption (hsa04961 )
- Pathways in cancer (hsa05200 )
- Proteoglycans in cancer (hsa05205 )
- Chemical carcinogenesis - receptor activation (hsa05207 )
- Breast cancer (hsa05224 )
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| Reactome Pathway |
- PIP3 activates AKT signaling (R-HSA-1257604 )
- Constitutive Signaling by Aberrant PI3K in Cancer (R-HSA-2219530 )
- Nuclear Receptor transcription pathway (R-HSA-383280 )
- SUMOylation of intracellular receptors (R-HSA-4090294 )
- Ovarian tumor domain proteases (R-HSA-5689896 )
- PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling (R-HSA-6811558 )
- TFAP2 (AP-2) family regulates transcription of growth factors and their receptors (R-HSA-8866910 )
- RUNX1 regulates estrogen receptor mediated transcription (R-HSA-8931987 )
- ESR-mediated signaling (R-HSA-8939211 )
- RUNX1 regulates transcription of genes involved in WNT signaling (R-HSA-8939256 )
- Regulation of RUNX2 expression and activity (R-HSA-8939902 )
- Extra-nuclear estrogen signaling (R-HSA-9009391 )
- Estrogen-dependent gene expression (R-HSA-9018519 )
- Nuclear signaling by ERBB4 (R-HSA-1251985 )
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