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Fulvestrant: an estrogen receptor antagonist that downregulates the estrogen receptor

Seminars in Oncology, 2003
Fulvestrant, a novel antiestrogen classified as an estrogen receptor antagonist without known agonist effects, was recently approved in the United States for the treatment of postmenopausal, hormone receptor-positive women with progressive metastatic breast cancer after antiestrogen therapy.
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Estrogen Receptors and Anti-Estrogen Therapies

2006
The realisation that breast cancer growth is regulated by the hormone estrogen led to the development of tamoxifen as the first target-directed cancer drug. Clearly, there is considerable headway to be made in further elucidating estrogen receptor function, in particular in identifying the mechanisms underlying endocrine resistance.
Lakjaya, Buluwela   +3 more
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Estrogen Receptor Action

Critical Reviews™ in Eukaryotic Gene Expression, 2002
Today we have to consider the existence of two estrogen receptors, alpha and beta, in our attempts to understand the role of estrogen receptors in physiology and pathology, and to explain the pharmacology of estrogens, antiestrogens, and SERMs. Both ERalpha and ERbeta belong to the large family of nuclear receptors that function as hormone-dependent ...
Stefan, Nilsson, Jan-Ake, Gustafsson
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Estrogen receptor phosphorylation

Steroids, 2003
Estrogen receptor alpha (ERalpha) is phosphorylated on multiple amino acid residues. For example, in response to estradiol binding, human ERalpha is predominately phosphorylated on Ser-118 and to a lesser extent on Ser-104 and Ser-106. In response to activation of the mitogen-activated protein kinase pathway, phosphorylation occurs on Ser-118 and Ser ...
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Estrogen Receptor Variants

Journal of Mammary Gland Biology and Neoplasia, 1998
Estrogen receptor (ER)3 gene expression in breast epithelium is an intricately regulated event. The human ER gene is transcribed from at least three different promoters which are expressed in a cell- and tissue-specific manner, and result in mRNA isoforms with unique 5'-untranslated exons.
T A, Hopp, S A, Fuqua
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Estrogen Receptor Assay

JAMA: The Journal of the American Medical Association, 1977
To the Editor.— Kiang and Kennedy (238:59-60, 1977) have presented an interesting idea that may prove to be useful in the differential diagnosis of adenocarcinomas of unknown primary site. Unfortunately, however, the evidence offered hardly appears to justify their claim that positive estrogen receptor assays can indicate that metastases arose from ...
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The standardization of estrogen receptors

The Journal of Steroid Biochemistry and Molecular Biology, 1993
Tumour estrogen receptor (ER) status may determine the medical treatment of a patient with breast cancer; yet inter-laboratory results can vary markedly, particularly when absolute cut-offs in fmol/mg cytosol protein are used. The use of standardized log units is proposed to permit greater inter-laboratory comparability.
Judy-Anne W. Chapman   +11 more
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The estrogen receptor family

Current Opinion in Obstetrics and Gynaecology, 1999
A significant flow of new data is currently being generated within the field of estrogen receptors and their mechanisms of action. This is primarily a result of the development of estrogen receptor knockout mice and the discovery of the second estrogen receptor, estrogen receptor beta.
M, Warner, S, Nilsson, J A, Gustafsson
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An update on estrogen receptors

Seminars in Perinatology, 2000
The discovery of a second estrogen receptor (ER), ERbeta, has led to a complete change in our views on estrogen action. The previous dogmatic view that ERalpha represented the only estrogen receptor led to a static and simplistic concept of mechanisms of estrogen action with conceptual limitations in the development of novel estrogenic and ...
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Transcriptional Suppression of the Estrogen Receptor by Truncated Estrogen Receptor-Alpha

Hormone and Metabolic Research, 2002
The estrogen receptor (ER) is composed of six major functional domains - the A/B domain as the activation function 1 domain, domain C as the DNA-binding domain, domain D as a hinge domain, and domain E/F as the ligand-dependent transcriptional domains. A novel protein (designated as SRB-RGS) that interacted with domains C and D of ER alpha (ER alpha C ...
M, Ikeda   +4 more
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