Identification of an Orally Bioavailable Chromene-Based Selective Estrogen Receptor Degrader (SERD) That Demonstrates Robust Activity in a Model of Tamoxifen-Resistant Breast Cancer

About 75% of breast cancers are estrogen receptor alpha (ER-α) positive, and women typically initially respond well to antihormonal therapies such as tamoxifen and aromatase inhibitors, but resistance often emerges. Fulvestrant is a steroid-based, selective estrogen receptor degrader (SERD) that bot...

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Veröffentlicht in:Journal of medicinal chemistry 2018-09, Vol.61 (17), p.7917-7928
Hauptverfasser: Nagasawa, Johnny, Govek, Steven, Kahraman, Mehmet, Lai, Andiliy, Bonnefous, Celine, Douglas, Karensa, Sensintaffar, John, Lu, Nhin, Lee, KyoungJin, Aparicio, Anna, Kaufman, Josh, Qian, Jing, Shao, Gang, Prudente, Rene, Joseph, James D, Darimont, Beatrice, Brigham, Daniel, Maheu, Kate, Heyman, Richard, Rix, Peter J, Hager, Jeffrey H, Smith, Nicholas D
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Sprache:eng
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