Structural underpinnings of oestrogen receptor mutations in endocrine therapy resistance

  title={Structural underpinnings of oestrogen receptor mutations in endocrine therapy resistance},
  author={John A. Katzenellenbogen and Christopher G. Mayne and Benita S Katzenellenbogen and Geoffrey L Greene and Sarat Chandarlapaty},
  journal={Nature Reviews Cancer},
Oestrogen receptor-α (ERα), a key driver of breast cancer, normally requires oestrogen for activation. Mutations that constitutively activate ERα without the need for hormone binding are frequently found in endocrine-therapy-resistant breast cancer metastases and are associated with poor patient outcomes. The location of these mutations in the ER ligand-binding domain and their impact on receptor conformation suggest that they subvert distinct mechanisms that normally maintain the low basal… CONTINUE READING

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