Reactome | ESTG translocates to the nucleus

ESTG translocates to the nucleus

Stable Identifier

R-HSA-8939205

Type

Reaction [omitted]

Species

Homo sapiens

Compartment

extracellular region, nucleoplasm

ReviewStatus

5/5

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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 Cosman, F, Lindsay, R	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 Hah, N, Kraus, WL	Mol. Cell. Endocrinol.	2014
16511588	Estrogen receptors and human disease Deroo, BJ, Korach, KS	J. Clin. Invest.	2006
11162936	Molecular mechanisms of estrogen action: selective ligands and receptor pharmacology Katzenellenbogen, BS, Choi, I, Delage-Mourroux, R, Ediger, TR, Martini, PG, Montano, M, Sun, J, Weis, K, Katzenellenbogen, JA	J. Steroid Biochem. Mol. Biol.	2000