Article
Discovery of Selective Estrogen Receptor Covalent Antagonists for the Treatment of ERαWT and ERαMUT Breast Cancer.
Cancer discovery - 1 Sept 2018
Puyang Xiaoling, Furman Craig, Zheng Guo Zhu, Wu Zhenhua J, Banka Deepti, Aithal Kiran, Agoulnik Sergei, Bolduc David M, Buonamici Silvia, Caleb Benjamin, Das Subhasree, Eckley Sean, Fekkes Peter, Hao Ming-Hong, Hart Andrew, Houtman René, Irwin Sean, Joshi Jaya J, Karr Craig, Kim Amy, Kumar Namita, Kumar Pavan, Kuznetsov Galina, Lai Weidong G, Larsen Nicholas, Mackenzie Crystal, Martin Lesley-Ann, Melchers Diana, Moriarty Alyssa, Nguyen Tuong-Vi, Norris John, O'Shea Morgan, Pancholi Sunil, Prajapati Sudeep, Rajagopalan Sujatha, Reynolds Dominic J, Rimkunas Victoria, Rioux Nathalie, Ribas Ricardo, Siu Amy, Sivakumar Sasirekha, Subramanian Vanitha, Thomas Michael, Vaillancourt Frédéric H, Wang John, Wardell Suzanne, Wick Michael J, Yao Shihua, Yu Lihua, Warmuth Markus, Smith Peter G, Zhu Ping, Korpal Manav
Abstract excerpt
Mutations in estrogen receptor alpha (ERα) that confer resistance to existing classes of endocrine therapies are detected in up to 30% of patients who have relapsed during endocrine treatments. Because a significant proportion of therapy-resistant breast cancer metastases continue to be dependent on ERα signaling, there remains a critical need to develop the next generation of ERα antagonists that can overcome...
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