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Identification of nonabsorbable inhibitors of the scavenger receptor-BI (SR-BI) for tissue-specific administration.
Sparks, Steven M; Zhou, Huiqiang; Generaux, Claudia; Harston, Lindsey; Moncol, David; Jayawickreme, Channa; Parham, Janet; Condreay, Patrick; Rimele, Thomas.
Afiliación
  • Sparks SM; GlaxoSmithKline, Enteroendocrine Discovery Performance Unit and Platform Technology and Science, 5 Moore Drive, Research Triangle Park, NC 27709, United States. Electronic address: ssparks@viamet.com.
  • Zhou H; GlaxoSmithKline, Enteroendocrine Discovery Performance Unit and Platform Technology and Science, 5 Moore Drive, Research Triangle Park, NC 27709, United States.
  • Generaux C; GlaxoSmithKline, Enteroendocrine Discovery Performance Unit and Platform Technology and Science, 5 Moore Drive, Research Triangle Park, NC 27709, United States.
  • Harston L; GlaxoSmithKline, Enteroendocrine Discovery Performance Unit and Platform Technology and Science, 5 Moore Drive, Research Triangle Park, NC 27709, United States.
  • Moncol D; GlaxoSmithKline, Enteroendocrine Discovery Performance Unit and Platform Technology and Science, 5 Moore Drive, Research Triangle Park, NC 27709, United States.
  • Jayawickreme C; GlaxoSmithKline, Enteroendocrine Discovery Performance Unit and Platform Technology and Science, 5 Moore Drive, Research Triangle Park, NC 27709, United States.
  • Parham J; GlaxoSmithKline, Enteroendocrine Discovery Performance Unit and Platform Technology and Science, 5 Moore Drive, Research Triangle Park, NC 27709, United States.
  • Condreay P; GlaxoSmithKline, Enteroendocrine Discovery Performance Unit and Platform Technology and Science, 5 Moore Drive, Research Triangle Park, NC 27709, United States.
  • Rimele T; GlaxoSmithKline, Enteroendocrine Discovery Performance Unit and Platform Technology and Science, 5 Moore Drive, Research Triangle Park, NC 27709, United States.
Bioorg Med Chem Lett ; 26(8): 1901-4, 2016 Apr 15.
Article en En | MEDLINE | ID: mdl-26988301
ABSTRACT
The identification of a low-permeability scavenger receptor BI (SR-BI) inhibitor starting from the ITX-5061 template is described. Structure-activity and structure-permeability relationships were assessed for analogs leading to the identification of compound 8 as a potent and nonabsorbable SR-BI inhibitor.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Fenilendiaminas / Sulfonamidas / Receptores Depuradores de Clase B Tipo de estudio: Diagnostic_studies Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2016 Tipo del documento: Article
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Fenilendiaminas / Sulfonamidas / Receptores Depuradores de Clase B Tipo de estudio: Diagnostic_studies Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2016 Tipo del documento: Article