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The SERM/SERD bazedoxifene disrupts ESR1 helix 12 to overcome acquired hormone resistance in breast cancer cells

Acquired resistance to endocrine therapy remains a significant clinical burden for breast cancer patients. Somatic mutations in the ESR1 (estrogen receptor alpha (ERα)) gene ligand-binding domain (LBD) represent a recognized mechanism of acquired resistance. Antiestrogens with improved efficacy vers...

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Detalles Bibliográficos
Autores principales: Fanning, Sean W, Jeselsohn, Rinath, Dharmarajan, Venkatasubramanian, Mayne, Christopher G, Karimi, Mostafa, Buchwalter, Gilles, Houtman, René, Toy, Weiyi, Fowler, Colin E, Han, Ross, Lainé, Muriel, Carlson, Kathryn E, Martin, Teresa A, Nowak, Jason, Nwachukwu, Jerome C, Hosfield, David J, Chandarlapaty, Sarat, Tajkhorshid, Emad, Nettles, Kendall W, Griffin, Patrick R, Shen, Yang, Katzenellenbogen, John A, Brown, Myles, Greene, Geoffrey L
Formato: Online Artículo Texto
Lenguaje:English
Publicado: eLife Sciences Publications, Ltd 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6335054/
https://www.ncbi.nlm.nih.gov/pubmed/30489256
http://dx.doi.org/10.7554/eLife.37161