Summary

Name ESR1
Full Name Estrogen receptor
Synonyms ER, ER-alpha, Estradiol receptor, Nuclear receptor subfamily 3 group A member 1 | ESR, NR3A1
Primary ID P03372
Links - -
Type protein
Relations 141
Pathways Luminal Breast Cancer, Oxytocin signaling
Inhibitors afimoxifene; fulvestrant; tamoxifen; raloxifene; hexestrol; tamoxifen citrate
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.

Viewer

Modifications Tables

Relations

Regulator Mechanism target score
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.34
Publications: 4 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.764
Publications: 4 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.669
Publications: 6 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.478
Publications: 4 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png phosphorylation ESR1 0.259
Publications: 3
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.702
Publications: 5 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.2
Publications: 4 Organism: Homo Sapiens
Pathways:Luminal Breast Cancer
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.419
Publications: 3 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.2
Publications: 3 Organism: Homo Sapiens
Pathways:Luminal Breast Cancer, Oxytocin signaling
+ up-regulates activity img/direct-activation.png phosphorylation ESR1 0.256
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.624
Publications: 2 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.306
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.414
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png phosphorylation ESR1 0.398
Publications: 1 Organism: Homo Sapiens
+ up-regulates quantity by stabilization img/direct-activation.png phosphorylation ESR1 0.386
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png phosphorylation ESR1 0.471
Publications: 1 Organism: Homo Sapiens
+ down-regulates activity img/direct_inhibition.png dephosphorylation ESR1 0.261
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.403
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.342
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png phosphorylation ESR1 0.357
Publications: 2 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png phosphorylation ESR1 0.51
Publications: 1 Organism: Chlorocebus Aethiops
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.494
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.2
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.593
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png phosphorylation ESR1 0.485
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png phosphorylation ESR1 0.246
Publications: 2 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.485
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png phosphorylation ESR1 0.277
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.535
Publications: 1 Organism: Homo Sapiens
Tissue: Breast
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.446
Publications: 2 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.383
Publications: 2 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.777
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png dephosphorylation ESR1 0.2
Publications: 1 Organism: Homo Sapiens
+ down-regulates activity img/direct_inhibition.png binding ESR1 0.2
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png chemical activation ESR1 0.8
Publications: 1 Organism: In Vitro
+ down-regulates quantity by repression img/indirect_inhibition.png transcriptional regulation ESR1 0.421
Publications: 1 Organism: Homo Sapiens
+ up-regulates quantity by expression img/indirect-activation.png transcriptional regulation KDM4B 0.605
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png chemical activation ESR1 0.8
Publications: 1 Organism: In Vitro
+ up-regulates activity img/direct-activation.png chemical activation ESR1 0.8
Publications: 1 Organism: In Vitro
+ up-regulates activity img/direct-activation.png chemical activation ESR1 0.8
Publications: 1 Organism: In Vitro
Pathways:Luminal Breast Cancer
+ up-regulates quantity by expression img/indirect-activation.png transcriptional regulation CDKN1A 0.478
Publications: 1 Organism: Homo Sapiens
+ down-regulates activity img/direct_inhibition.png chemical inhibition ESR1 0.8
Publications: 1 Organism: In Vitro
+ up-regulates img/direct-activation.png binding PIK3R2 0.544
Publications: 1 Organism: Homo Sapiens
+ up-regulates quantity by expression img/direct-activation.png transcriptional regulation CRH 0.34
Publications: 1 Organism: Homo Sapiens
Tissue: Hypothalamus
+ up-regulates quantity by expression img/direct-activation.png transcriptional regulation CCND1 0.753
Publications: 1 Organism: Homo Sapiens
+ down-regulates activity img/indirect_inhibition.png ESR1 0.753
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png chemical activation ESR1 0.8
Publications: 1 Organism: In Vitro
+ up-regulates img/direct-activation.png chemical activation ESR1 0.8
Publications: 1 Organism: Homo Sapiens
Pathways:Luminal Breast Cancer
+ down-regulates activity img/direct_inhibition.png chemical inhibition ESR1 0.8
Publications: 1 Organism: Homo Sapiens
+ down-regulates quantity by repression img/indirect_inhibition.png transcriptional regulation ESR1 0.399
Publications: 1 Organism: Homo Sapiens
+ up-regulates quantity by expression img/indirect-activation.png transcriptional regulation GREB1 0.713
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png chemical activation ESR1 0.8
Publications: 1 Organism: In Vitro
+ down-regulates quantity by repression img/indirect_inhibition.png transcriptional regulation ESR1 0.656
Publications: 1 Organism: Homo Sapiens
+ down-regulates activity img/direct_inhibition.png deubiquitination ESR1 0.545
Publications: 1
+ down-regulates quantity by repression img/direct_inhibition.png transcriptional regulation CYP19A1 0.516
Publications: 1
Pathways:Luminal Breast Cancer
+ up-regulates quantity by expression img/indirect-activation.png transcriptional regulation UGT1A4 0.299
Publications: 1 Organism: Homo Sapiens
+ down-regulates quantity by repression img/indirect_inhibition.png transcriptional regulation NR0B2 0.648
Publications: 1 Organism: Homo Sapiens
+ up-regulates quantity by expression img/indirect-activation.png transcriptional regulation F12 0.2
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PI3K 0.66
Publications: 1 Organism: Homo Sapiens
+ down-regulates activity img/direct_inhibition.png transcriptional regulation ESR1 0.291
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding ESR1 0.845
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png binding ESR1 0.57
Publications: 1 Organism: Homo Sapiens
+ down-regulates quantity by repression img/indirect_inhibition.png transcriptional regulation SCN11A 0.2
Publications: 1 Organism: Mus Musculus
Tissue: Spinal Ganglion
+ down-regulates quantity img/direct_inhibition.png phosphorylation ESR1 0.434
Publications: 1 Organism: Homo Sapiens
+ up-regulates quantity by expression img/indirect-activation.png transcriptional regulation NCOA2 0.818
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png phosphorylation ESR1 0.499
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png binding ESR1 0.552
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png chemical activation ESR1 0.8
Publications: 1 Organism: In Vitro
+ up-regulates quantity by expression img/indirect-activation.png transcriptional regulation OXT 0.426
Publications: 1 Organism: Homo Sapiens
Pathways:Oxytocin signaling
+ up-regulates activity img/direct-activation.png chemical activation ESR1 0.8
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png binding ESR1 0.648
Publications: 1 Organism: Homo Sapiens
Tissue: Ovary
+ img/unknown.png transcriptional regulation MYC 0.728
Publications: 1 Organism: Homo Sapiens
+ up-regulates quantity by expression img/indirect-activation.png transcriptional regulation SCN8A 0.2
Publications: 1 Organism: Mus Musculus
+ up-regulates quantity by expression img/indirect-activation.png transcriptional regulation TGFA 0.526
Publications: 1 Organism: Homo Sapiens
+ down-regulates activity img/direct_inhibition.png chemical inhibition ESR1 0.8
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3R1 0.627
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png chemical activation ESR1 0.8
Publications: 2 Organism: In Vitro
+ down-regulates quantity by repression img/indirect_inhibition.png transcriptional regulation SNAI2 0.421
Publications: 1 Organism: Homo Sapiens
+ down-regulates quantity by repression img/indirect_inhibition.png transcriptional regulation SCN10A 0.289
Publications: 1 Organism: Mus Musculus
Tissue: Spinal Ganglion
+ up-regulates activity img/direct-activation.png chemical activation ESR1 0.8
Publications: 1 Organism: In Vitro
+ down-regulates activity img/direct_inhibition.png chemical inhibition ESR1 0.8
Publications: 1 Organism: In Vitro
+ down-regulates quantity by repression img/indirect_inhibition.png transcriptional regulation ESR1 0.389
Publications: 2 Organism: Homo Sapiens
+ down-regulates quantity img/direct_inhibition.png ubiquitination ESR1 0.427
Publications: 1 Organism: Homo Sapiens
+ down-regulates activity img/direct_inhibition.png chemical inhibition ESR1 0.8
Publications: 1 Organism: In Vitro
+ up-regulates quantity by expression img/direct-activation.png transcriptional regulation ESR1 0.25
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.2
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.572
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png chemical activation ESR1 0.8
Publications: 1 Organism: In Vitro
+ down-regulates quantity by repression img/direct_inhibition.png transcriptional regulation PPARG 0.28
Publications: 1 Organism: Homo Sapiens
+ down-regulates quantity by repression img/indirect_inhibition.png transcriptional regulation SCN9A 0.2
Publications: 1 Organism: Mus Musculus
Tissue: Spinal Ganglion
+ down-regulates activity img/direct_inhibition.png chemical inhibition ESR1 0.8
Publications: 1 Organism: Homo Sapiens
+ down-regulates quantity by repression img/indirect_inhibition.png transcriptional regulation AR 0.416
Publications: 1 Organism: Homo Sapiens
+ up-regulates quantity by expression img/indirect-activation.png transcriptional regulation TFF1 0.752
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png binding AP1 0.72
Publications: 1 Organism: Homo Sapiens
Pathways:Luminal Breast Cancer
+ up-regulates activity img/direct-activation.png chemical activation ESR1 0.8
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.59
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding ESR1 0.623
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png chemical activation ESR1 0.8
Publications: 1 Organism: In Vitro
+ down-regulates quantity by repression img/indirect_inhibition.png transcriptional regulation PGR 0.623
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding ESR1 0.456
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png chemical activation ESR1 0.8
Publications: 1 Organism: In Vitro
+ down-regulates quantity by repression img/indirect_inhibition.png transcriptional regulation SCN1A 0.267
Publications: 1 Organism: Mus Musculus
Tissue: Spinal Ganglion
+ down-regulates quantity by repression img/indirect_inhibition.png transcriptional regulation SCN5A 0.2
Publications: 1 Organism: Homo Sapiens
Tissue: Spinal Ganglion
+ up-regulates img/direct-activation.png binding ESR2 0.526
Publications: 1 Organism: Homo Sapiens
Pathways:Oxytocin signaling
+ up-regulates quantity by expression img/indirect-activation.png transcriptional regulation PSEN2 0.28
Publications: 1
+ up-regulates img/direct-activation.png binding ESR1 0.455
Publications: 1 Organism: Homo Sapiens
+ down-regulates quantity by destabilization img/direct_inhibition.png ubiquitination ESR1 0.345
Publications: 1 Organism: Homo Sapiens