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Estrogen Receptors alpha and beeta Two Receptors of a Kind

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Ever since the discovery of estradiol and the elucidation of its chemical structure, there has been a great deal of interest in its mechanism of action and its potential therapeutic value. It is now well established that estrogens have many different functions in many different cell-types. With respect to the potential use of estrogens as therapeutics, there is an interest in controlling reproductive function, bone metabolism, cardiovascular disease, as well as in the prevention of hot flushes, mood changes and Alzheimers disease. For over a decade, it was believed that estrogens signal through a a single estrogen receptor, now referred to as ER alpha, which belongs to a family of ligand-activated transcription factors. More recently, however, a second estrogen receptor ERb was identified. The current review describes similarities as well as differences between these two distinct estrogen receptors. Both ER alpha and ER beeta bind 17beeta-estradiol with high affinity and they bind to classical estrogen response elements in a similar if not identical fashion. However, there are also major differences between ER alpha and ERbeeta for instance with respect to their tissue distribution, the phenotype of the corresponding knock-out mice and their transcriptional activities. It is anticipated that a better understanding of these two receptors will eventually lead to more selective ways of modulating physiological processes which are influenced by estrogens. For this purpose, the development of ERa and ERb specific ligands, both agonists as well as antagonists, will be of great importance.
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Keywords: DNA binding domain DBD; MAPK mediated serine phosphorylation; Splice variants; agonists antagonsits; anti estrogen 4 hydroxytamoxifen OHT; estrogen receptor; glucocorticoid GR; high throughput screening assays; hormone replacement therapy; ligand binding specificity; ligand independent activation; nuclear receptor gene; transcriptional co regualtors

Document Type: Review Article

Publication date: May 1, 2000

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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