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Identification of potent, nonabsorbable agonists of the calcium-sensing receptor for GI-specific administration.
Sparks, Steven M; Spearing, Paul K; Diaz, Caroline J; Cowan, David J; Jayawickreme, Channa; Chen, Grace; Rimele, Thomas J; Generaux, Claudia; Harston, Lindsey T; Roller, Shane G.
Afiliação
  • Sparks SM; Enteroendocrine Discovery Performance Unit and Platform Technologies and Science, GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, United States. Electronic address: ssparks@viamet.com.
  • Spearing PK; Enteroendocrine Discovery Performance Unit and Platform Technologies and Science, GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, United States.
  • Diaz CJ; Enteroendocrine Discovery Performance Unit and Platform Technologies and Science, GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, United States.
  • Cowan DJ; Enteroendocrine Discovery Performance Unit and Platform Technologies and Science, GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, United States.
  • Jayawickreme C; Enteroendocrine Discovery Performance Unit and Platform Technologies and Science, GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, United States.
  • Chen G; Enteroendocrine Discovery Performance Unit and Platform Technologies and Science, GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, United States.
  • Rimele TJ; Enteroendocrine Discovery Performance Unit and Platform Technologies and Science, GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, United States.
  • Generaux C; Enteroendocrine Discovery Performance Unit and Platform Technologies and Science, GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, United States.
  • Harston LT; Enteroendocrine Discovery Performance Unit and Platform Technologies and Science, GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, United States.
  • Roller SG; Enteroendocrine Discovery Performance Unit and Platform Technologies and Science, GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, United States.
Bioorg Med Chem Lett ; 27(20): 4673-4677, 2017 10 15.
Article em En | MEDLINE | ID: mdl-28916340
ABSTRACT
Modulation of gastrointestinal nutrient sensing pathways provides a promising a new approach for the treatment of metabolic diseases including diabetes and obesity. The calcium-sensing receptor has been identified as a key receptor involved in mineral and amino acid nutrient sensing and thus is an attractive target for modulation in the intestine. Herein we describe the optimization of gastrointestinally restricted calcium-sensing receptor agonists starting from a 3-aminopyrrolidine-containing template leading to the identification of GI-restricted agonist 19 (GSK3004774).
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Texto completo: 1 Bases de dados: MEDLINE Assunto principal: Receptores de Detecção de Cálcio Tipo de estudo: Diagnostic_studies / Prognostic_studies Limite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2017 Tipo de documento: Article
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Bases de dados: MEDLINE Assunto principal: Receptores de Detecção de Cálcio Tipo de estudo: Diagnostic_studies / Prognostic_studies Limite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2017 Tipo de documento: Article