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Potent and Orally Bioavailable GPR142 Agonists as Novel Insulin Secretagogues for the Treatment of Type 2 Diabetes.
Toda, Narihiro; Hao, Xiaolin; Ogawa, Yasuyuki; Oda, Kozo; Yu, Ming; Fu, Zice; Chen, Yi; Kim, Yongjae; Lizarzaburu, Mike; Lively, Sarah; Lawlis, Shauna; Murakoshi, Michiko; Nara, Futoshi; Watanabe, Nobuaki; Reagan, Jeff D; Tian, Hui; Fu, Angela; Motani, Alykhan; Liu, Qingxiang; Lin, Yi-Jyun; Zhuang, Run; Xiong, Yumei; Fan, Peter; Medina, Julio; Li, Leping; Izumi, Masanori; Okuyama, Ryo; Shibuya, Satoshi.
Afiliação
  • Toda N; Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.
  • Hao X; Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.
  • Ogawa Y; Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.
  • Oda K; Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.
  • Yu M; Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.
  • Fu Z; Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.
  • Chen Y; Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.
  • Kim Y; Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.
  • Lizarzaburu M; Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.
  • Lively S; Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.
  • Lawlis S; Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.
  • Murakoshi M; Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.
  • Nara F; Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.
  • Watanabe N; Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.
  • Reagan JD; Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.
  • Tian H; Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.
  • Fu A; Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.
  • Motani A; Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.
  • Liu Q; Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.
  • Lin YJ; Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.
  • Zhuang R; Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.
  • Xiong Y; Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.
  • Fan P; Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.
  • Medina J; Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.
  • Li L; Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.
  • Izumi M; Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.
  • Okuyama R; Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.
  • Shibuya S; Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.
ACS Med Chem Lett ; 4(8): 790-4, 2013 Aug 08.
Article em En | MEDLINE | ID: mdl-24900747
GPR142 is a G protein-coupled receptor that is predominantly expressed in pancreatic ß-cells. GPR142 agonists stimulate insulin secretion in the presence of high glucose concentration, so that they could be novel insulin secretagogues with reduced or no risk of hypoglycemia. We report here the optimization of HTS hit compound 1 toward a proof of concept compound 33, which showed potent glucose lowering effects during an oral glucose tolerance test in mice and monkeys.
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Texto completo: 1 Base de dados: MEDLINE Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2013 Tipo de documento: Article País de afiliação: Japão
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2013 Tipo de documento: Article País de afiliação: Japão