[Specific modulators of estrogen action].
Selective estradiol receptor modulators (SERMs) are specific modulators of estradiol action. They are used in therapeutics to obtain an estrogenic effect on certain cells and an antiestrogenic effect on other cells. Recent progress in the knowledge of the mechanism of action of estradiols implies that new molecules could be designed. This progress involves the cloning of a new estradiol receptor, ER beta, the discovery of co-activators and the elucidation of their molecular mechanism of action, and the crystallization of the ligand binding domain in the presence of an agonist or an antagonist.
Guiochon-Mantel
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Inserm U 135, laboratoire d'hormonologie et biologie moléculaire, hôpital de Bicêtre, Le Kremlin, France.
D000818:Animals; D004958:Estradiol / Q000494:pharmacology; D006801:Humans; D011960:Receptors, Estrogen / Q000032:analysis / Q000235:genetics / Q000502:physiology; D020845:Selective Estrogen Receptor Modulators / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use
D011960:Receptors, Estrogen; D020845:Selective Estrogen Receptor Modulators; D004958:Estradiol