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Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts.
Lai, Andiliy; Kahraman, Mehmet; Govek, Steven; Nagasawa, Johnny; Bonnefous, Celine; Julien, Jackie; Douglas, Karensa; Sensintaffar, John; Lu, Nhin; Lee, Kyoung-Jin; Aparicio, Anna; Kaufman, Josh; Qian, Jing; Shao, Gang; Prudente, Rene; Moon, Michael J; Joseph, James D; Darimont, Beatrice; Brigham, Daniel; Grillot, Kate; Heyman, Richard; Rix, Peter J; Hager, Jeffrey H; Smith, Nicholas D.
Afiliación
  • Lai A; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States.
  • Kahraman M; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States.
  • Govek S; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States.
  • Nagasawa J; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States.
  • Bonnefous C; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States.
  • Julien J; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States.
  • Douglas K; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States.
  • Sensintaffar J; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States.
  • Lu N; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States.
  • Lee KJ; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States.
  • Aparicio A; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States.
  • Kaufman J; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States.
  • Qian J; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States.
  • Shao G; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States.
  • Prudente R; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States.
  • Moon MJ; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States.
  • Joseph JD; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States.
  • Darimont B; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States.
  • Brigham D; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States.
  • Grillot K; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States.
  • Heyman R; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States.
  • Rix PJ; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States.
  • Hager JH; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States.
  • Smith ND; †Department of Chemistry, ‡Department of Biology, §Department of Drug Safety and Disposition, Seragon Pharmaceuticals, 12780 El Camino Real, Suite 302, San Diego, California 92130, United States.
J Med Chem ; 58(12): 4888-904, 2015 Jun 25.
Article en En | MEDLINE | ID: mdl-25879485
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Tamoxifeno / Neoplasias de la Mama / Moduladores Selectivos de los Receptores de Estrógeno / Receptor alfa de Estrógeno / Bibliotecas de Moléculas Pequeñas / Proteolisis / Antineoplásicos Tipo de estudio: Diagnostic_studies Límite: Animals / Female / Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2015 Tipo del documento: Article País de afiliación: Estados Unidos
Texto completo
Imprimir
XML
PubMed Links
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Tamoxifeno / Neoplasias de la Mama / Moduladores Selectivos de los Receptores de Estrógeno / Receptor alfa de Estrógeno / Bibliotecas de Moléculas Pequeñas / Proteolisis / Antineoplásicos Tipo de estudio: Diagnostic_studies Límite: Animals / Female / Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2015 Tipo del documento: Article País de afiliación: Estados Unidos