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New options for breast cancer drug development found in estrogen receptors

October 09, 2018 / Case Western Reserve University

Many breast cancer drugs block estrogen receptors inside cancer cells. Blocking the receptors early in disease progression staves off metastasis. But most patients with advanced disease eventually develop drug resistance, leaving doctors desperate for alternatives. Now, researchers from Case Western Reserve University School of Medicine have uncovered a previously uncharacterized, bridge-like structure within the human estrogen receptor that could serve as a valuable new drug target. In Nature Communications, researchers describe a "burning the bridge" strategy to disrupting the estrogen receptor, and how to screen breast cancer drugs designed to do it. "Until now, the structure of the entire estrogen receptor complex was unknown, so it was a challenge to identify novel or functionally important target sites for new drugs," said Sichun Yang, Ph.D., senior author on the study and associate professor of nutrition, proteomics, pharmacology, and biophysics at Case Weste...