Characterization of molecular and structural determinants of selective estrogen receptor downregulators

@article{Fan2006CharacterizationOM,
  title={Characterization of molecular and structural determinants of selective estrogen receptor downregulators},
  author={Meiyun Fan and Emily L. Rickert and Lei Chen and Syed Arafat Aftab and Kenneth P. Nephew and Ross V. Weatherman},
  journal={Breast Cancer Research and Treatment},
  year={2006},
  volume={103},
  pages={37-44}
}
Antiestrogens used for breast cancer therapy can be categorized into two classes that differ in their effect on estrogen receptor (ER) alpha stability. The selective estrogen receptor modulators (SERMs) stabilize ER alpha and the selective estrogen receptor downregulators (SERDs) cause a decrease in cellular ER alpha levels. A clinically relevant antiestrogen, GW7604, appears to work through a SERD-like mechanism, despite sharing the same molecular scaffold as 4-hydroxytamoxifen, a SERM. In… CONTINUE READING

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