Point mutation of estrogen receptor (ER) in the ligand-binding domain changes the pharmacology of antiestrogens in ER-negative breast cancer cells stably expressing complementary DNAs for ER.

@article{Jiang1992PointMO,
  title={Point mutation of estrogen receptor (ER) in the ligand-binding domain changes the pharmacology of antiestrogens in ER-negative breast cancer cells stably expressing complementary DNAs for ER.},
  author={Shu Ye Jiang and Susan M. Langan-Fahey and Attilio L. Stella and Ray McCague and V. Craig Jordan},
  journal={Molecular endocrinology},
  year={1992},
  volume={6 12},
  pages={2167-74}
}
The antiestrogen tamoxifen is used in the treatment of hormone-responsive breast cancer. However, therapeutic failure has frequently been observed in both patients and animal models after long term treatment. We have studied the effect of a point mutation that leads to the substitution of Val for Gly at codon 400 in the ligand-binding domain of the estrogen receptor (ER) on estrogenic and antiestrogenic activities of 4-hydroxytamoxifen (4-OHT) and its derivatives. Stable ER transfectants… CONTINUE READING

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Tamoxifen Resistance in Breast Cancer

Biomolecules & therapeutics • 2012
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