Conformational Changes and Coactivator Recruitment by Novel Ligands for Estrogen Receptor-α and Estrogen Receptor-β: Correlations with Biological Character and Distinct Differences among SRC Coactivator Family Members.

@article{Kraichely2000ConformationalCA,
  title={Conformational Changes and Coactivator Recruitment by Novel Ligands for Estrogen Receptor-α and Estrogen Receptor-β: Correlations with Biological Character and Distinct Differences among SRC Coactivator Family Members.},
  author={Dennis M Kraichely and Jun Sun and John A. Katzenellenbogen and Benita S Katzenellenbogen},
  journal={Endocrinology},
  year={2000},
  volume={141 10},
  pages={3534-3545}
}
Ligands for the estrogen receptor (ER) that have the capacity to selectively bind to or activate the ER subtypes ERa or ERb would be useful in elucidating the biology of these two receptors and might assist in the development of estrogen pharmaceuticals with improved tissue selectivity. In this study, we examine three compounds of novel structure that act as ER subtype-selective ligands. These are a propyl pyrazole triol (PPT), which is a potent agonist on ERa but is inactive on ERb, and a pair… CONTINUE READING

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Er Subtype Ligands and Coactivator Recruitment

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For personal use only. No other uses without permission. . All rights reserved • 2000

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