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Discovery of a novel potent GPR40 full agonist.
Meegalla, Sanath K; Huang, Hui; Martin, Tonya; Xu, June; Zhao, Shuyuan; Liu, Jianying; Hall, Meghan; Gunnet, Joe; Wang, Yuanping; Rady, Brian; Silva, Jose; Otieno, Monicah; Arnoult, Eric; Paul Lee, S; Pocai, Alessandro; Player, Mark R.
Afiliação
  • Meegalla SK; CVM Discovery, Janssen Research & Developmen, LLC, Welsh and McKean Roads, Spring House, PA 19477-0776, USA.
  • Huang H; CVM Discovery, Janssen Research & Developmen, LLC, Welsh and McKean Roads, Spring House, PA 19477-0776, USA.
  • Martin T; CVM Discovery, Janssen Research & Developmen, LLC, Welsh and McKean Roads, Spring House, PA 19477-0776, USA.
  • Xu J; CVM Discovery, Janssen Research & Developmen, LLC, Welsh and McKean Roads, Spring House, PA 19477-0776, USA.
  • Zhao S; CVM Discovery, Janssen Research & Developmen, LLC, Welsh and McKean Roads, Spring House, PA 19477-0776, USA.
  • Liu J; CVM Discovery, Janssen Research & Developmen, LLC, Welsh and McKean Roads, Spring House, PA 19477-0776, USA.
  • Hall M; CVM Discovery, Janssen Research & Developmen, LLC, Welsh and McKean Roads, Spring House, PA 19477-0776, USA.
  • Gunnet J; CVM Discovery, Janssen Research & Developmen, LLC, Welsh and McKean Roads, Spring House, PA 19477-0776, USA.
  • Wang Y; CVM Discovery, Janssen Research & Developmen, LLC, Welsh and McKean Roads, Spring House, PA 19477-0776, USA.
  • Rady B; CVM Discovery, Janssen Research & Developmen, LLC, Welsh and McKean Roads, Spring House, PA 19477-0776, USA.
  • Silva J; PDS-TPL-TOX, Janssen Research & Development, LLC, Welsh and McKean Roads, Spring House, PA 19477-0776, USA.
  • Otieno M; PDS-TPL-TOX, Janssen Research & Development, LLC, Welsh and McKean Roads, Spring House, PA 19477-0776, USA.
  • Arnoult E; Computational Chemistry, Janssen Research & Development, LLC, Welsh and McKean Roads, Spring House, PA 19477-0776, USA.
  • Paul Lee S; CVM Discovery, Janssen Research & Developmen, LLC, Welsh and McKean Roads, Spring House, PA 19477-0776, USA.
  • Pocai A; CVM Discovery, Janssen Research & Developmen, LLC, Welsh and McKean Roads, Spring House, PA 19477-0776, USA.
  • Player MR; CVM Discovery, Janssen Research & Developmen, LLC, Welsh and McKean Roads, Spring House, PA 19477-0776, USA. Electronic address: mplayer@its.jnj.com.
Bioorg Med Chem Lett ; 28(4): 720-726, 2018 02 15.
Article em En | MEDLINE | ID: mdl-29366647
ABSTRACT
Compound 12 is a GPR40 agonist that realizes the full magnitude of efficacy possible via GPR40 receptor agonism. In vitro and in vivo studies demonstrated superior glucose lowering by 12 compared to fasiglifam (TAK-875), in a glucose dependent manner. The enhanced efficacy observed with the full agonist 12 was associated with both direct and indirect stimulation of insulin secretion.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirazinas / Receptores Acoplados a Proteínas G / Hipoglicemiantes Limite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2018 Tipo de documento: Article País de afiliação: Estados Unidos
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirazinas / Receptores Acoplados a Proteínas G / Hipoglicemiantes Limite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2018 Tipo de documento: Article País de afiliação: Estados Unidos