Regulation of specific target genes and biological responses by estrogen receptor subtype agonists
- Author(s)
- Leitman, DC; Paruthiyil, S; Vivar, OI; Saunier, EF; Herber, CB; Cohen, I; Tagliaferri, M; Speed, TP;
- Details
- Publication Year 2010-12,Volume 10,Issue #6,Page 629-636
- Journal Title
- CURRENT OPINION IN PHARMACOLOGY
- Publication Type
- Journal Article
- Abstract
- Estrogenic effects are mediated through two estrogen receptor (ER) subtypes, ER alpha and ER beta Estrogens are the most commonly prescribed drugs to treat menopausal conditions but by non-selectively triggering both ER alpha and ER beta pathways in different tissues they can cause serious adverse effects The different sizes of the binding pockets and sequences of their activation function domains indicate that ER alpha and ER beta should have different specificities for ligands and biological responses that can be exploited for designing safer and more selective estrogens ER alpha and ER beta regulate different genes by binding to different regulatory elements and recruiting different transcription and chromatin remodeling factors that are expressed in a cell-specific manner ER alpha-selective and ER beta-selective agonists have been identified that demonstrate that the two ERs produce distinct biological effects ER alpha and ER beta agonists are a promising new approach for treating specific conditions associated with menopause
- Publisher
- ELSEVIER SCI LTD
- Keywords
- MENOPAUSAL HOT FLUSHES; ER-ALPHA; BETA-AGONIST; MOLECULAR-MECHANISMS; OSTEOSARCOMA CELLS; SELECTIVE LIGANDS; BINDING-SITES; PROLIFERATION; TRANSCRIPTION; EXPRESSION
- Publisher's Version
- https://doi.org/10.1016/j.coph.2010.09.009
- Terms of Use/Rights Notice
- Refer to copyright notice on published article.
Creation Date: 2010-12-01 12:00:00