ESTG translocates to the nucleus

Stable Identifier
Reaction [omitted]
Homo sapiens
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Extracellular estrogens diffuse freely across the plasma membrane and into the nucleus. In the nucleus, estrogens interact with estrogen receptors and, in conjunction with other transcriptional regulators, promote changes in estrogen-responsive transcription (reviewed in Hall et al, 2001; Deroo and Korach, 2006; Hah and Kraus, 2014). The estrogen receptor binds endogenous estrogens such as 17 beta estradiol (E2, the most potent ligand), estrone (E1), estriol (E3) and estretol (E4), as well as other physiological ligands such as oxysterols derivatives like 27-hydroxycholesterol (reviewed in Arnal, 2017; Nguyen et al, 2015; Nelson et al, 2013). In addition to naturally occurring ligands, there are many other synthetic estrogen ligands in clinical use that bind the estrogen receptor and modulate biological response. These include agonists, which mimic the effect of naturally occurring estrogens, mixed agonist-antagonists (also known as selective estrogen receptor modulators, or SERMs, which show tissue-specific activities) and antagonists (reviewed in Cosman and Lindsay, 1999; Katzenellenbogen et al, 2000; Bai and Gust, 2009; Farooq, 2015).
Literature References
PubMed ID Title Journal Year
11459850 The multifaceted mechanisms of estradiol and estrogen receptor signaling

Hall, JM, Couse, JF, Korach, KS

J. Biol. Chem. 2001
25866274 Structural and Functional Diversity of Estrogen Receptor Ligands

Farooq, A

Curr Top Med Chem 2015
10368777 Selective estrogen receptor modulators: clinical spectrum

Lindsay, R, Cosman, F

Endocr. Rev. 1999
19274700 Breast cancer, estrogen receptor and ligands

Bai, Z, Gust, R

Arch. Pharm. (Weinheim) 2009
23810978 Hormone-regulated transcriptomes: lessons learned from estrogen signaling pathways in breast cancer cells

Kraus, WL, Hah, N

Mol. Cell. Endocrinol. 2014
16511588 Estrogen receptors and human disease

Korach, KS, Deroo, BJ

J. Clin. Invest. 2006
11162936 Molecular mechanisms of estrogen action: selective ligands and receptor pharmacology

Katzenellenbogen, JA, Montano, M, Katzenellenbogen, BS, Choi, I, Sun, J, Ediger, TR, Weis, K, Delage-Mourroux, R, Martini, PG

J. Steroid Biochem. Mol. Biol. 2000
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