NR3

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].
Corticosteroid receptors include mineralocorticoid (MR) and glucocorticoid (GR) receptors. They play a crucial role in the regulation of a variety of physiological processes, including reproduction, metabolism, salt balance, inflammation, and immunity. Cortisol is the principal glucocorticoid that induces the transcriptional activities of both the GR and MR, whereas the mineralocorticoid aldosterone also activates only MR, but not GR[3].
The MR belongs to the cytosolic receptor family where the ligand diffuses into cells, interacts with the receptor and results in a signal transduction affecting specific gene expression in the nucleus. The GR, however, upon activation may up-regulate the expression of anti-inflammatory proteins in the nucleus or repress the expression of pro-inflammatory proteins in the cytosol by preventing the translocation of other transcription factors from the cytosol into the nucleus. In the absence of hormone, the MR and GR reside in the cytosol complexed with a variety of proteins including heat shock protein 70 and 90 (hsp70, hsp90), high-mobility group box proteins (HMGBs), and FKBP52 (FK506-binding protein 52)[4].


[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.
[3] Dissecting mineralocorticoid receptor structure and function. F.M. Rogerson, F.E. Brennan, P.J. Fuller. J Steroid Biochem. Mol. Biol. 2003, 85, 389-396. 
[4] Mechanisms of Mineralocorticoid Action. P.J. Fuller, M.J. Young. Hypertension 2005, 46, 1227-1235. 

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Axon ID Name Description From price
1979 ARN 509 Antagonist of androgen receptor (AR) €95.00
1675 Asoprisnil Progesterone receptor (PR) modulator €120.00
1748 Bazedoxifene hydrochloride Selective estrogen receptor modulator (SERM) €80.00
1426 Ciclesonide Glucocorticoid €65.00
1427 Diflorasone Diacetate Corticosteroid €95.00
1428 Difluprednate Corticosteroid €75.00
1232 DPN Estrogen (ER-β) agonist €70.00
2190 Endoxifen Selective estrogen receptor modulator (SERM) €125.00
2707 Endoxifen hydrochloride Selective estrogen receptor modulator (SERM) €125.00
2221 Endoxifen, (Z)- The more active (Z)-isomer of Endoxifen (SERM; Axon 2190) €155.00
1898 ERB 041 Selective estrogen receptor β (ERβ) agonist €95.00
1926 Estetrol Estrogen receptor agonist, (four- to five-fold preference for the Erα) €95.00
1169 Flumethasone Selective and potent glucocorticoid receptor agonist €60.00
2247 Flumethasone pivalate Topical glucocorticoid receptor agonist €60.00
1429 Flunisolide Corticosteroid €95.00

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