Receptor nomenclature | NR3A1 |
Receptor code | 4.10.1:EST:3:A1 |
Other names | ER1, Esr1 |
Molecular information | Hs: 595aa, P03372, chr. 6q251 |
| Rn: 600aa, P06211, chr. 1q122 |
| Mm: 599aa, P19785, chr. 10 A13 |
DNA binding | |
Structure | Homodimer |
HRE core sequence | GGTCAnnnTGACC (ERE, half-site, palindrome) |
Partners | HSP90 (physical, functional): cellular localization, DNA binding4; AP1 (physical, functional): DNA binding, transcriptional activition5; SP1 (physical, functional): DNA binding, transcriptional activation6 |
Agonists | Diethylstilbestrol (0.04 nM), 4-hydroxytamoxifen* (0.14 nM), 17β-estradiol* (0.15 nM), propylpyrazole triol (0.23 nM), raloxifen (0.31 nM), estriol (2.2 nM), estrone (3.2 nM), (R,R)-THC (4.2 nM), tamoxifen* (15 nM) [Ki]7–9 |
Antagonists | Hexestrol (0.05 nM), 4-OH-tamoxifen* (0.14 nM), raloxifen (0.31 nM), ICI182780 (0.24 nM), tamoxifen* (15 nM) [Ki]7 |
Coactivators | NCOA1, NCOA2, NCOA3, CREBBP, PPARBP, P68, SRA10 |
Corepressors | NCOR1, NRIP110 |
Biologically important isoforms | ERα46 {Hs}: translation is started at an internal ATG and produces a protein that lacks most of AF111; A908 {Hs}: mutation appears in premalignant breast lesions and malignant breast cancers12 |
Tissue distribution | Endometrium, liver, white adipose tissue, breast, bone, central and peripheral nervous system, ovary, cardiovascular system, brain, testis, prostate, epididymis {Hs, Mm, Rn} [Northern blot, Q-PCR, in situ hybridization, Western blot, immunohistology] |
Functional assays | Uterotrophic assay {Mm, Rn}13; HGP axis (gonadotropin suppression) {Hs, Mm, Rn}14; vaginal cornification {Mm, Rn}15 |
Main target genes | Activated: pS2 {Hs}16, progesterone receptor {Hs}17, cathepsin D {Hs}18 |
Mutant phenotype | Obesity, insulin resistance, diabetes, infertility (male and female), uterine atrophy, female loss of negative gonadotropin feedback, loss of female sexual and maternal behavior, genu valgum, elevated gonadotropins, autoimmune glomerularnephritis, osteopenia, cardiovascular vasodilation resistance {Mm} [knockout]19 |
Human disease | Breast cancer20; endometrial cancer21; obesity22; insulin resistance and diabetes22 |