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Intimate estrogen receptor-α/ligand relationships signal biological activity.

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How does estrogen receptor-α bind its natural ligands - estrogens? How can other molecules mimic estrogens and elicit different estrogenic responses? The answers lie in a complex and intimate chemical… Click to show full abstract

How does estrogen receptor-α bind its natural ligands - estrogens? How can other molecules mimic estrogens and elicit different estrogenic responses? The answers lie in a complex and intimate chemical biology between ligands and receptor. This delicate interaction at the ligand binding cleft signals, via conformational change, exposure of a specific new charge topography at a second site (Activation Function-2). This, in turn, attracts a regulatory protein which modulates gene expression and controls biological activity.

Keywords: biological activity; intimate; estrogen receptor

Journal Title: Toxicology
Year Published: 2018

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