Covalent ERα Antagonist H3B-6545 Demonstrates Encouraging Preclinical Activity in Therapy-Resistant Breast Cancer

Nearly 30% of patients with relapsed breast cancer present activating mutations in estrogen receptor alpha (ERα) that confer partial resistance to existing endocrine-based therapies. We previously reported the development of H3B-5942, a covalent ERα antagonist that engages cysteine-530 (C530) to ach...

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Detalles Bibliográficos
Autores principales: Furman, Craig, Puyang, Xiaoling, Zhang, Zhaojie, Wu, Zhenhua J., Banka, Deepti, Aithal, Kiran B., Albacker, Lee A., Hao, Ming-Hong, Irwin, Sean, Kim, Amy, Montesion, Meagan, Moriarty, Alyssa D., Murugesan, Karthikeyan, Nguyen, Tuong-Vi, Rimkunas, Victoria, Sahmoud, Tarek, Wick, Michael J., Yao, Shihua, Zhang, Xun, Zeng, Hao, Vaillancourt, Frédéric H., Bolduc, David M., Larsen, Nicholas, Zheng, Guo Zhu, Prajapati, Sudeep, Zhu, Ping, Korpal, Manav
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Association for Cancer Research 2022
Materias:
Small Molecule Therapeutics
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9381127/
https://www.ncbi.nlm.nih.gov/pubmed/35642432
http://dx.doi.org/10.1158/1535-7163.MCT-21-0378

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