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 108
Pathways Luminal Breast Cancer
Inhibitors tamoxifen citrate; fulvestrant; raloxifene; tamoxifen; hexestrol; afimoxifene
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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Modifications Tables

Relations

Regulator Mechanism target score
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.14
Publications: 4 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.14
Publications: 3 Organism: Homo Sapiens
Pathways:Luminal Breast Cancer
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.14
Publications: 4 Organism: Homo Sapiens
Pathways:Luminal Breast Cancer
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.23
Publications: 6 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.2
Publications: 4 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.2
Publications: 5 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.14
Publications: 4 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.14
Publications: 3 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.14
Publications: 1 Organism: Homo Sapiens
+ down-regulates activity img/direct_inhibition.png dephosphorylation ESR1 0.14
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.2
Publications: 2 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.14
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.14
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png phosphorylation ESR1 0.14
Publications: 1 Organism: Chlorocebus Aethiops
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.14
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.14
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.14
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.14
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png phosphorylation ESR1 0.14
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png phosphorylation ESR1 0.14
Publications: 2 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.14
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.14
Publications: 1 Organism: Homo Sapiens
Tissue: Breast
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.14
Publications: 2 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.34
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.2
Publications: 2 Organism: Homo Sapiens
+ img/unknown.png transcriptional regulation MYC 0.14
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding ESR1 0.41
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png chemical activation ESR1 0.14
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.14
Publications: 1 Organism: Homo Sapiens
+ down-regulates quantity by repression img/indirect_inhibition.png transcriptional regulation SCN11A 0.14
Publications: 1 Organism: Mus Musculus
Tissue: Spinal Ganglion
+ down-regulates quantity by repression img/indirect_inhibition.png transcriptional regulation SCN1A 0.14
Publications: 1 Organism: Mus Musculus
Tissue: Spinal Ganglion
+ down-regulates quantity by repression img/indirect_inhibition.png transcriptional regulation SCN9A 0.14
Publications: 1 Organism: Mus Musculus
Tissue: Spinal Ganglion
+ down-regulates quantity by repression img/indirect_inhibition.png transcriptional regulation ESR1 0.14
Publications: 1 Organism: Homo Sapiens
+ down-regulates quantity by repression img/indirect_inhibition.png transcriptional regulation ESR1 0.14
Publications: 1 Organism: Homo Sapiens
+ up-regulates quantity by expression img/indirect-activation.png transcriptional regulation GREB1 0.14
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png chemical activation ESR1 0.14
Publications: 1 Organism: Homo Sapiens
+ down-regulates activity img/direct_inhibition.png chemical inhibition ESR1 0.14
Publications: 1 Organism: Homo Sapiens
+ down-regulates activity img/direct_inhibition.png chemical inhibition ESR1 0.14
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png chemical activation ESR1 0.2
Publications: 1 Organism: Homo Sapiens
+ down-regulates quantity by repression img/indirect_inhibition.png transcriptional regulation AR 0.14
Publications: 1 Organism: Homo Sapiens
+ down-regulates quantity by repression img/indirect_inhibition.png transcriptional regulation ESR1 0.14
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding ESR2 0.45
Publications: 1 Organism: Homo Sapiens
+ down-regulates activity img/direct_inhibition.png transcriptional regulation ESR1 0.14
Publications: 1 Organism: Homo Sapiens
+ down-regulates activity img/indirect_inhibition.png ESR1 0.14
Publications: 1 Organism: Homo Sapiens
+ down-regulates quantity by repression img/indirect_inhibition.png transcriptional regulation SNAI2 0.14
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3R2 0.14
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding ESR1 0.3
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png binding ESR1 0.34
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PI3K 0.14
Publications: 1 Organism: Homo Sapiens
+ down-regulates activity img/direct_inhibition.png chemical inhibition ESR1 0.14
Publications: 1 Organism: In Vitro
+ up-regulates activity img/direct-activation.png chemical activation ESR1 0.14
Publications: 1 Organism: In Vitro
+ up-regulates activity img/direct-activation.png chemical activation ESR1 0.14
Publications: 1 Organism: In Vitro
+ down-regulates activity img/direct_inhibition.png chemical inhibition ESR1 0.14
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png chemical activation ESR1 0.2
Publications: 1 Organism: In Vitro
+ down-regulates activity img/direct_inhibition.png chemical inhibition ESR1 0.14
Publications: 1 Organism: In Vitro
+ down-regulates activity img/direct_inhibition.png chemical inhibition ESR1 0.14
Publications: 1 Organism: In Vitro
+ up-regulates activity img/direct-activation.png chemical activation ESR1 0.14
Publications: 1 Organism: In Vitro
+ up-regulates activity img/direct-activation.png chemical activation ESR1 0.14
Publications: 1 Organism: In Vitro
+ down-regulates quantity by repression img/indirect_inhibition.png transcriptional regulation SCN10A 0.14
Publications: 1 Organism: Mus Musculus
Tissue: Spinal Ganglion
+ up-regulates quantity by expression img/indirect-activation.png transcriptional regulation SCN8A 0.14
Publications: 1 Organism: Mus Musculus
+ down-regulates quantity by repression img/indirect_inhibition.png transcriptional regulation PGR 0.28
Publications: 1 Organism: Homo Sapiens
+ up-regulates quantity by expression img/indirect-activation.png transcriptional regulation TGFA 0.14
Publications: 1 Organism: Homo Sapiens
+ up-regulates quantity by expression img/indirect-activation.png transcriptional regulation TFF1 0.14
Publications: 1 Organism: Homo Sapiens
+ up-regulates quantity by expression img/indirect-activation.png transcriptional regulation CDKN1A 0.14
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding ESR1 0.14
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png binding ESR1 0.31
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png binding ESR1 0.14
Publications: 1 Organism: Homo Sapiens
Tissue: Ovary
+ up-regulates img/direct-activation.png binding PIK3R1 0.4
Publications: 1 Organism: Homo Sapiens
+ up-regulates quantity by expression img/indirect-activation.png transcriptional regulation F12 0.14
Publications: 1 Organism: Homo Sapiens
+ down-regulates quantity by repression img/indirect_inhibition.png transcriptional regulation NR0B2 0.14
Publications: 1 Organism: Homo Sapiens
+ down-regulates quantity by repression img/direct_inhibition.png transcriptional regulation PPARG 0.14
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding ESR1 0.35
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png phosphorylation ESR1 0.28
Publications: 1 Organism: Homo Sapiens
+ down-regulates quantity by repression img/indirect_inhibition.png transcriptional regulation ESR1 0.2
Publications: 2 Organism: Homo Sapiens
+ up-regulates quantity by expression img/indirect-activation.png transcriptional regulation NCOA2 0.36
Publications: 1 Organism: Homo Sapiens
+ up-regulates quantity by expression img/direct-activation.png transcriptional regulation CCND1 0.14
Publications: 1 Organism: Homo Sapiens
+ down-regulates quantity by repression img/indirect_inhibition.png transcriptional regulation SCN5A 0.14
Publications: 1 Organism: Homo Sapiens
Tissue: Spinal Ganglion
+ up-regulates quantity by expression img/indirect-activation.png transcriptional regulation UGT1A4 0.14
Publications: 1 Organism: Homo Sapiens