Estrogen Receptor α Activation
Estrogen receptor α (ERα), a member of the steroid receptor superfamily, contains highly conserved DNA binding and ligand binding domains. Through its estrogen-independent and estrogen-dependent activation domains (Estrogen receptor αAF-1 and AF-2, respectively), ERα regulates transcription by recruiting coactivator proteins and interacting with general transcriptional machinery. Phosphorylation at multiple sites provides an important mechanism to regulate ERα activity.
Ser104, 106, 118, and 167 are located in the amino-terminal transcription activation function domain AF-1, and phosphorylation of these serine residues plays an important role in regulating ERα activity. Ser118 may be the substrate of the transcription regulatory kinase CDK7. Ser167 may be phosphorylated by p90RSK and Akt. According to the research literature, phosphorylation at Ser167 may confer tamoxifen resistance in breast cancer patients.
The role of estrogen receptor alpha and estrogen receptor alpha antagonists (tamoxifen, fulvestrant, letrozole, and anastrozole) in breast cancer
Relevant Antibodies
| Catalog# | Product Name | Reactivity | Application |
|---|---|---|---|
| AMRe21336 | Histone H3 Rabbit Monoclonal antibody | Human,Mouse,Rat | WB,IHC,IF,IP,ELISA |
| AMRe03979 | DiMethyl-Histone H3 (Lys79) Rabbit Monoclonal Antibody | Human, Mouse, Rat | WB,IHC-F,IHC-P,ICC/IF |
| AMRe84137 | Histone H3(monomethylK79) Rabbit Monoclonal Antibody | Human,Mouse,Rat | WB,IP,IHC,ICC,IF |
| APS0635 | HRP-conjugated Polyclonal Goat Anti-Rabbit IgG(H+L) Secondary Antibody | Rabbit | ELISA, WB, Dot blot |
| APS0631 | HRP-conjugated Polyclonal Goat Anti-Mouse IgG(H+L) Secondary Antibody | Mouse | ELISA, WB, Dot blot |
| AMre80004 | GAPDH (12R9) Rabbit Monoclonal Antibody | Human,Mouse,Rat,Rabbit,Dog,Monkey | WB,ELISA |
Related Products
References
- Mangelsdorf DJ, Thummel C, Beato M, et,al. The nuclear receptor superfamily: the second decade. Cell. 1995 Dec 15;83(6):835-9. doi: 10.1016/0092-8674(95)90199-x. [PMID: 8521507].
- Glass CK, Rosenfeld MG. The coregulator exchange in transcriptional functions of nuclear receptors. Genes Dev. 2000 Jan 15;14(2):121-41. [PMID: 10652267].
- Chen D, Pace PE, Coombes RC, Ali S. Phosphorylation of human estrogen receptor alpha by protein kinase A regulates dimerization. Mol Cell Biol. 1999 Feb;19(2):1002-15.[PMID: 9891036].
- Campbell RA, Bhat-Nakshatri P, Patel NM, Constantinidou D, et,al. Phosphatidylinositol 3-kinase/AKT-mediated activation of estrogen receptor alpha: a new model for anti-estrogen resistance. J Biol Chem. 2001 Mar 30;276(13):9817-24. Epub 2001 Jan 3. [PMID: 11139588].
- Chen D, Riedl T, Washbrook E, Pace PE, Coombes RC, Egly JM, Ali S. Activation of estrogen receptor alpha by S118 phosphorylation involves a ligand-dependent interaction with TFIIH and participation of CDK7. Mol Cell. 2000 Jul;6(1):127-37. [PMID: 10949034].
- Joel PB, Smith J, Sturgill TW, et,al. pp90rsk1 regulates estrogen receptor-mediated transcription through phosphorylation of Ser-167. Mol Cell Biol. 1998 Apr;18(4):1978-84. [ PMID: 9528769].
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