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Novel Sulfonanilide Inhibitors of SHIP2 Enhance Glucose Uptake into Cultured Myotubes.
Berg, Mika E A; Naams, Jette-Britt; Hautala, Laura C; Tolvanen, Tuomas A; Ahonen, Jari P; Lehtonen, Sanna; Wähälä, Kristiina.
Afiliación
  • Berg MEA; Department of Chemistry, University of Helsinki, A. I. Virtasen aukio 1, 00014 Helsinki, Finland.
  • Naams JB; Research Program for Clinical and Molecular Metabolism, Faculty of Medicine, University of Helsinki, Haartmaninkatu 3, Helsinki, 00014 Finland.
  • Hautala LC; Research Program for Clinical and Molecular Metabolism, Faculty of Medicine, University of Helsinki, Haartmaninkatu 3, Helsinki, 00014 Finland.
  • Tolvanen TA; Department of Pathology, University of Helsinki, Haartmaninkatu 3, 00014 Helsinki, Finland.
  • Ahonen JP; Department of Chemistry, University of Helsinki, A. I. Virtasen aukio 1, 00014 Helsinki, Finland.
  • Lehtonen S; Research Program for Clinical and Molecular Metabolism, Faculty of Medicine, University of Helsinki, Haartmaninkatu 3, Helsinki, 00014 Finland.
  • Wähälä K; Department of Pathology, University of Helsinki, Haartmaninkatu 3, 00014 Helsinki, Finland.
ACS Omega ; 5(3): 1430-1438, 2020 Jan 28.
Article en En | MEDLINE | ID: mdl-32010815
A series of substituted sulfonanilide analogs were prepared and evaluated as novel potent inhibitors of SH2 domain-containing inositol polyphosphate 5'-phosphatase 2 (SHIP2). SHIP2 has been shown to be a new attractive target for the treatment of insulin resistance in type 2 diabetes mellitus (T2D), which can lead to life-threatening diabetic kidney disease (DKD). Amongst the synthesized compounds, the two most promising candidates, 10 and 11, inhibited SHIP2 significantly. Additionally, these compounds induced Akt activation in a dose-dependent manner, increased the presence of glucose transporter 4 at the plasma membrane, and enhanced glucose uptake in cultured myotubes in vitro at lower concentrations than metformin, the most widely used antidiabetic drug. These results show that the novel SHIP2 inhibitors have insulin sensitizing capacity and provide prototypes for further drug development for T2D and DKD.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: ACS Omega Año: 2020 Tipo del documento: Article País de afiliación: Finlandia Pais de publicación: Estados Unidos
Texto completo
Añadir a Mi BVS
Imprimir
XML
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: ACS Omega Año: 2020 Tipo del documento: Article País de afiliación: Finlandia Pais de publicación: Estados Unidos