Binding characteristics of novel nonsteroidal antiestrogens to the rat uterine estrogen receptors.

@article{Martel1998BindingCO,
  title={Binding characteristics of novel nonsteroidal antiestrogens to the rat uterine estrogen receptors.},
  author={Ce Line Martel and Louis Provencher and Xing-wang Li and A M St Pierre and G{\'e}rard Leblanc and Sylvain Gauthier and Yves M{\'e}rand and Fernand Labrie},
  journal={The Journal of steroid biochemistry and molecular biology},
  year={1998},
  volume={64 3-4},
  pages={199-205}
}
Tamoxifen (TAM), the only antiestrogen currently available for the endocrine therapy of breast cancer behaves as a mixed agonist/antagonist of estrogen action, thus limiting its therapeutic potential. We report the binding characteristics of a novel series of nonsteroidal antiestrogens to the rat uterine estrogen receptor. As measured by competition studies, the affinity of EM-652, the active metabolite of the prodrug EM-800, for the estrogen receptor is 7-11 times higher than that of 17beta… CONTINUE READING