Intimate estrogen receptor-α/ligand relationships signal biological activity

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.