Estrogen Receptor alpha

Publication Title: 
The Journal of Biological Chemistry

Estrogen receptors (ER alpha/ER beta) are expressed in neuronal cells and exhibit a variety of activities in the central nervous system. ER activity is regulated in a ligand-dependent manner and by co-regulatory factors. Caveolin-1 is a recently identified co-activator of ER alpha mediating the ligand-independent activation of this steroid receptor. Here the influence of ERs on caveolin expression in human neuroblastoma SK-N-MC cells as well as in rodent brain was investigated.

Author(s): 
Zschocke, J¸rgen
Manthey, Dieter
Bayatti, Nadhim
van der Burg, Bart
Goodenough, Sharon
Behl, Christian
Publication Title: 
Oncotarget

Hormone-dependent gene expression requires dynamic and coordinated epigenetic changes. Estrogen receptor-positive (ER+) breast cancer is particularly dependent upon extensive chromatin remodeling and changes in histone modifications for the induction of hormone-responsive gene expression. Our previous studies established an important role of bromodomain-containing protein-4 (BRD4) in promoting estrogen-regulated transcription and proliferation of ER+ breast cancer cells.

Author(s): 
Nagarajan, Sankari
Benito, Eva
Fischer, Andre
Johnsen, Steven A.
Publication Title: 
Carcinogenesis

MCF7 cells are an estrogen-responsive human breast cancer cell line that expresses both estrogen receptor (ER) alpha and ERbeta. Treatment of MCF7 cells with artemisinin, an antimalarial phytochemical from the sweet wormwood plant, effectively blocked estrogen-stimulated cell cycle progression induced by either 17beta-estradiol (E(2)), an agonist for both ERs, or by propyl pyrazole triol (PPT), a selective ERalpha agonist. Artemisinin strongly downregulated ERalpha protein and transcripts without altering expression or activity of ERbeta.

Author(s): 
Sundar, Shyam N.
Marconett, Crystal N.
Doan, Victor B.
Willoughby, Jamin A.
Firestone, Gary L.
Publication Title: 
Molecular Carcinogenesis

We have shown previously that withaferin A (WA), a promising anticancer constituent of Ayurvedic medicine plant Withania somnifera, inhibits growth of MCF-7 and MDA-MB-231 human breast cancer cells in culture and MDA-MB-231 xenografts in vivo by causing apoptosis. However, the mechanism of WA-induced apoptosis is not fully understood. The present study was designed to systematically determine the role of tumor suppressor p53 and estrogen receptor-α (ER-α) in proapoptotic response to WA using MCF-7, T47D, and ER-α overexpressing MDA-MB-231 cells as a model.

Author(s): 
Hahm, Eun-Ryeong
Lee, Joomin
Huang, Yi
Singh, Shivendra V.
Publication Title: 
Molecular Carcinogenesis

We have shown previously that withaferin A (WA), a promising anticancer constituent of Ayurvedic medicine plant Withania somnifera, inhibits growth of MCF-7 and MDA-MB-231 human breast cancer cells in culture and MDA-MB-231 xenografts in vivo by causing apoptosis. However, the mechanism of WA-induced apoptosis is not fully understood. The present study was designed to systematically determine the role of tumor suppressor p53 and estrogen receptor-α (ER-α) in proapoptotic response to WA using MCF-7, T47D, and ER-α overexpressing MDA-MB-231 cells as a model.

Author(s): 
Hahm, Eun-Ryeong
Lee, Joomin
Huang, Yi
Singh, Shivendra V.
Publication Title: 
Journal of Agricultural and Food Chemistry

Because the prevailing form of hormone replacement therapy is associated with the development of cancer in breast and endometrial tissues, alternatives are needed for the management of menopausal symptoms. Formulations of Trifolium pratense L. (red clover) are being used to alleviate menopause-associated hot flashes but have shown mixed results in clinical trials. The strobiles of Humulus lupulusL.

Author(s): 
Overk, Cassia R.
Yao, Ping
Chadwick, Lucas R.
Nikolic, Dejan
Sun, Yongkai
Cuendet, Muriel A.
Deng, Yunfan
Hedayat, A. S.
Pauli, Guido F.
Farnsworth, Norman R.
van Breemen, Richard B.
Bolton, Judy L.
Publication Title: 
Anticancer Research

The peripheral-type benzodiazepine receptor (PBR) is an 18-kDa high affinity drug- and cholesterol-binding protein that is involved in various cell functions, including cell proliferation and apoptosis. PBR was shown to be overexpressed in certain types of malignant human tumors and cancer cell lines, correlating with enhanced tumorigenicity and cell proliferation rates. The present study was conducted in order to further define the role of PBR in cancer and to extend our recent findings regarding the possible anticancer effects of the standardized Ginkgo biloba extract EGb 761.

Author(s): 
Pretner, Ewald
Amri, Hakima
Li, Wenping
Brown, Rachel
Lin, Chin-Shoou
Makariou, Erini
Defeudis, Francis V.
Drieu, Katy
Papadopoulos, Vassilios
Publication Title: 
Journal of Alternative and Complementary Medicine (New York, N.Y.)

OBJECTIVES: To document the chemical and biologic profile of a clinical phase II red clover (Trifolium pratense L.) extract by identifying and measuring the major and minor components visible in the high-performance liquid chromatography-ultraviolet (HPLC-UV) chromatogram and evaluating each compound for estrogenic and antioxidant activity.

Author(s): 
Booth, Nancy L.
Overk, Cassia R.
Yao, Ping
Burdette, Joanna E.
Nikolic, Dejan
Chen, Shao-Nong
Bolton, Judy L.
van Breemen, Richard B.
Pauli, Guido F.
Farnsworth, Norman R.
Publication Title: 
Molecular and Cellular Endocrinology

After the Women's Health Initiative found that the risks of hormone therapy outweighed the benefits, a need for alternative drugs to treat menopausal symptoms has emerged. We explored the possibility that botanical agents used in Traditional Chinese Medicine for menopausal symptoms contain ERbeta-selective estrogens. We previously reported that an extract containing 22 herbs, MF101 has ERbeta-selective properties. In this study we isolated liquiritigenin, the most active estrogenic compound from the root of Glycyrrhizae uralensis Fisch, which is one of the plants found in MF101.

Author(s): 
Mersereau, Jennifer E.
Levy, Nitzan
Staub, Richard E.
Baggett, Scott
Zogovic, Tatjana
Zogric, Tetjana
Chow, Sylvia
Ricke, William A.
Tagliaferri, Mary
Cohen, Isaac
Bjeldanes, Leonard F.
Leitman, Dale C.
Publication Title: 
Combinatorial Chemistry & High Throughput Screening

A high throughput screening assay for the identification of ligands to pharmacologically significant receptors was developed based on magnetic particles containing immobilized receptors followed by liquid chromatography-mass spectrometry (LC-MS). This assay is suitable for the screening of complex mixtures such as botanical extracts. For proof-of-principle, estrogen receptor-alpha (ER-alpha) and ER-beta were immobilized on magnetic particles functionalized with aldehyde or carboxylic acid groups.

Author(s): 
Choi, Yongsoo
van Breemen, Richard B.

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