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Identification of a Potent and Selective GPR4 Antagonist as a Drug Lead for the Treatment of Myocardial Infarction.
Fukuda, Hayato; Ito, Saki; Watari, Kenji; Mogi, Chihiro; Arisawa, Mitsuhiro; Okajima, Fumikazu; Kurose, Hitoshi; Shuto, Satoshi.
Afiliação
  • Fukuda H; Faculty of Pharmaceutical Science, Hokkaido University , Kita-12, Nishi-6, Kita-Ku, Sapporo 060-0812, Japan.
  • Ito S; Faculty of Pharmaceutical Science, Hokkaido University , Kita-12, Nishi-6, Kita-Ku, Sapporo 060-0812, Japan.
  • Watari K; Department of Pharmacology and Toxicology, Graduate School of Pharmaceutical Sciences, Kyushu University , 3-1-1 Maidashi, Higashi-ku, Fukuoka 812-8582, Japan.
  • Mogi C; Laboratory of Signal Transduction, Institute for Molecular and Cellular Regulation, Gunma University , 3-39-15 Showa-machi, Maebashi 371-8512, Japan.
  • Arisawa M; Faculty of Pharmaceutical Science, Hokkaido University , Kita-12, Nishi-6, Kita-Ku, Sapporo 060-0812, Japan.
  • Okajima F; Laboratory of Signal Transduction, Institute for Molecular and Cellular Regulation, Gunma University , 3-39-15 Showa-machi, Maebashi 371-8512, Japan.
  • Kurose H; Department of Pharmacology and Toxicology, Graduate School of Pharmaceutical Sciences, Kyushu University , 3-1-1 Maidashi, Higashi-ku, Fukuoka 812-8582, Japan.
  • Shuto S; Faculty of Pharmaceutical Science, Hokkaido University, Kita-12, Nishi-6, Kita-Ku, Sapporo 060-0812, Japan; Center for Research and Education on Drug Discovery, Hokkaido University, Kita-12, Nishi-6, Kita-Ku, Sapporo 060-0812, Japan.
ACS Med Chem Lett ; 7(5): 493-7, 2016 May 12.
Article em En | MEDLINE | ID: mdl-27190599
GPR4, a pH-sensing G protein-coupled receptor, is highly expressed in endothelial cells and may be activated in myocardial infarction due the decreased tissue pH. We are interested in GPR4 antagonists as potential effective pharmacologic tools and/or drug leads for the treatment of myocardial infarction. We investigated the structure-activity relationship of a known GPR4 antagonist 1 as a lead compound to identify 3b as the first potent and selective GPR4 antagonist, whose effectiveness was demonstrated in a mouse myocardial infarction model.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Tipo de estudo: Diagnostic_studies Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2016 Tipo de documento: Article País de afiliação: Japão País de publicação: Estados Unidos
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Tipo de estudo: Diagnostic_studies Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2016 Tipo de documento: Article País de afiliação: Japão País de publicação: Estados Unidos