Estrogen (ER)
The third class of nuclear receptors (Nuclear, Class 3, Estrogen Receptor-like) includes estrogen and estrogen-related receptors (ER), as well as the 3-ketosteroid receptors (progesterone (PR), androgen (AR), gluco- and mineralocorticoid (GR and MR, respectively) receptors).
Estrogen is a key regulator of growth, differentiation and function in a broad range of target tissues, including the male and female reproductive tracts, mammary gland, bone, brain and the cardiovascular system. The biological effects of estrogen are mediated through estrogen receptors α and β (ERα, β). The classical mechanism of activation of ERs depends on ligand binding to the receptors, after which the receptors dimerize and bind to estrogen response elements (EREs) located in the promoters of estrogen-responsive genes. ERs may also regulate gene expression in the absence of DNA-binding by modulating the activities of other transcription factors via protein-protein interactions on DNA. This mechanism is referred to as cross-talk and is common for several nuclear receptors[1]. As the name implies, the family of estrogen receptor-related receptors (ERRs) is a subfamily of the orphan nuclear receptors, which is closely related to the estrogen receptor (ER) family, and comprises three subtypes (ERRα-γ). Sequence analyses comparing all the class 3 NRs have shown that both ERs and ERRs together form the same branch of class 3, which recognizes a specific hormone response element (HRE), whereas the other four steroid receptors (PR, AR, GR, and MR) recognize a different, yet specific HRE, thereby forming another branch[2].
[1] Estrogen receptor-dependent activation of AP-1 via non-genomic signaling. L. Björnström, M. Sjöberg. Nuclear Receptor 2004, 2, 3.
[2] The Orphan Nuclear Receptors, Estrogen Receptor-related Receptors: their Role as New Biomarkers in Gynecological Cancer. P. Sun, L. Wei, C. Denkert, W. Lichtenegger, J. Sehouli. Anticancer Res. 2006, 26 (2C), 1699-1706.
Axon ID | Name | Description | From price | |
---|---|---|---|---|
3704 | (S)-ErSO | Inactive enantiomer of ErSO | €180.00 | |
4093 | (Z)-4-Hydroxytamoxifen | The more active metabolite of Tamoxifen (SERM; Axon 3252) | €110.00 | |
2221 | (Z)-Endoxifen | The more active (Z)-isomer of Endoxifen (SERM; Axon 2190) | €150.00 | |
2051 | Bazedoxifene acetate | Selective estrogen receptor modulator (SERM) | €80.00 | |
1748 | Bazedoxifene hydrochloride | Selective estrogen receptor modulator (SERM) | €70.00 | |
2790 | BHPI | ER-α antagonist | €125.00 | |
3650 | Clomiphene citrate | Selective estrogen receptor modulator (SERM) | €50.00 | |
3322 | Dehydroepiandrosterone | Endogenous steroid hormone precursor | €60.00 | |
3320 | Diethylstilbestrol | Estrogen receptor agonist | €50.00 | |
1232 | DPN | Estrogen (ER-β) agonist | €70.00 | |
4095 | Elacestrant dihydrochloride | Orally bioavailable selective estrogen receptor degrader (SERD) | €220.00 | |
2190 | Endoxifen | Selective estrogen receptor modulator (SERM) | €125.00 | |
2707 | Endoxifen hydrochloride | Selective estrogen receptor modulator (SERM) | €130.00 | |
1898 | ERB 041 | Selective estrogen receptor β (ERβ) agonist | €95.00 | |
3594 | ErSO | Orally bioavailable a-UPR activator | €180.00 | |
1926 | Estetrol | Estrogen receptor agonist (four- to five-fold preference for the Erα) | €130.00 | |
1231 | PPT | ER-α agonist | €95.00 | |
3250 | Raloxifene | Selective estrogen receptor modulator (SERM) | €50.00 | |
3252 | Tamoxifen | Selective estrogen receptor modulator (SERM) | €50.00 | |
2697 | WAY-200070 | Brain penetrant ERβ-selective agonist | €105.00 | |
2652 | ZB716 | Steroidal, orally bioavailable SERD | €130.00 | |
4212 | α-Estradiol | Endogenous estrogen receptor ligand | Recently added | €90.00 |