Figure 7
Structural understanding of how agonists and antagonists mediate their effects on the estrogen receptor. (A) Both estradiol and the synthetic molecule diethylstilbestrol (DES) are agonists, whereas tamoxifen and raloxifene are antagonists. The antagonists differ from stilbesterol only in the addition of the extension moiety (in blue). (B) DES binding places helix-12 (H12) in the agonist conformation, as does estradiol. (C) The extension moiety in raloxifene pushes H12 out of its active conformation.
