Results 241 to 250 of about 2,614,131 (297)

Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer.

Journal of Medicinal Chemistry, 2018
In breast cancer, estrogen receptor alpha (ERα) positive cancer accounts for approximately 74% of all diagnoses, and in these settings, it is a primary driver of cell proliferation.
G. Tria, T. Abrams, J. Baird, H. Burks, B. Firestone, L. Gaither, L. Hamann, Guo He, C. Kirby, Sunkyu Kim, F. Lombardo, Kaitlin J Macchi, D. McDonnell, Y. Mishina, J. Norris, Jill Nunez, C. Springer, Yingchuan Sun, Noel M. Thomsen, Chunrong Wang, Jianling Wang, Bing Yu, Choi-Lai Tiong-Yip, S. Peukert   +23 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-Åke Gustafsson
openaire   +3 more sources

Gene expression and benefit of chemotherapy in women with node-negative, estrogen receptor-positive breast cancer.

Journal of Clinical Oncology, 2006
PURPOSE The 21-gene recurrence score (RS) assay quantifies the likelihood of distant recurrence in women with estrogen receptor-positive, lymph node-negative breast cancer treated with adjuvant tamoxifen.
S. Paik, G. Tang, S. Shak, Chungyeul Kim, J. Baker, W. Kim, M. Cronin, F. Baehner, D. Watson, J. Bryant, J. Costantino, C. Geyer, D. Wickerham, N. Wolmark   +13 more
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Estrogen receptor mutations

Molecular and Cellular Endocrinology, 1998
The purpose of this paper is to review potential novel functional pathways by which estradiol and estrogenic compounds elicit biological responses in mammals. We will limit our approach to those novel functions suggested by phenotypes associated with estrogen receptor-alpha (ER alpha) gene mutations and polymorphisms.
Dennis B. Lubahn, Julia A. Taylor, Kendall J Lewis   +2 more
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Estrogen receptors in the pancreas

Journal of Steroid Biochemistry, 1974
Minced rat pancreas retained a large portion of estradiol (E2) after incubation with either 5 nM or 1 μM concentrations of radioactive E2. The mince was homogenized in low salt buffer and separated into nuclei, mitochondria, microsomes, and cytosol by centrifugations at 1000 g, 10,000 g, and 105,000 g, respectively.
Hannah E. Rosenthal, Avery A. Sandberg
openaire   +2 more sources

Estrogen or estrogen receptor?

Trends in Endocrinology & Metabolism, 2003
View Large Image | Download PowerPoint SlideAs a clinical breast oncologist, I was eager to review Endocrine Therapy in Breast Cancer. Hormonal manipulation has been the predominant form of breast cancer treatment for >50 years. Surgical ablation, high-dose estrogens, LHRH agonists and antiestrogens have all shown clinical benefit.
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Estrogen receptor phosphorylation [PDF]

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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Activation of the Estrogen Receptor Through Phosphorylation by Mitogen-Activated Protein Kinase

Science, 1995
The phosphorylation of the human estrogen receptor (ER) serine residue at position 118 is required for full activity of the ER activation function 1 (AF-1).
S. Kato, H. Endoh, Y. Masuhiro, T. Kitamoto, Shimami Uchiyama, H. Sasaki, S. Masushige, Y. Gotoh, E. Nishida, H. Kawashima, D. Metzger, P. Chambon   +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.
Stefan Nilsson, Margaret Warner, Jan-Ake Gustafsson   +2 more
openaire   +3 more sources

Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts.

Journal of Medicinal Chemistry, 2015
Approximately 80% of breast cancers are estrogen receptor alpha (ER-α) positive, and although women typically initially respond well to antihormonal therapies such as tamoxifen and aromatase inhibitors, resistance often emerges.
Andiliy G. Lai, M. Kahraman, S. Govek, Johnny Y. Nagasawa, C. Bonnefous, J. Julien, Karensa L Douglas, J. Sensintaffar, Nhin Lu, Kyoung-jin Lee, Anna Aparicio, Josh Kaufman, J. Qian, G. Shao, R. Prudente, Michael J Moon, James D. Joseph, B. Darimont, D. Brigham, Kate Grillot, R. Heyman, P. Rix, J. Hager, N. Smith   +23 more
semanticscholar   +1 more source