Different positioning of the ligand-binding domain helix 12 and the F domain of the estrogen receptor accounts for functional differences between agonists and antagonists.

@article{Nichols1998DifferentPO,
  title={Different positioning of the ligand-binding domain helix 12 and the F domain of the estrogen receptor accounts for functional differences between agonists and antagonists.},
  author={Mark I Nichols and Jeanette M J Rientjes and Alexandre F. R. Stewart},
  journal={The EMBO journal},
  year={1998},
  volume={17 3},
  pages={765-73}
}
The estrogen receptor is capable of binding a diverse set of ligands that are broadly categorized as agonists or antagonists, depending on their abilities to induce or interfere with transcriptional responsiveness. We show, using a fusion protein assay for ligand-binding which does not rely on transcriptional responsiveness, that agonists and antagonists differently position the C-terminus of the ligand-binding domain (helix 12) and the F domain. Upon antagonist binding, the F domain interferes… CONTINUE READING
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