Novel compounds reducing IRS-1 serine phosphorylation for treatment of diabetes

Simon-Szabo, Laura; Kokas, Marton; Greff, Zoltan; Boros, Sandor; Banhegyi, Peter; Zsakai, Lilian; Szantai-Kis, Csaba; Vantus, Tibor; Mandl, Jazsef; Banhegyi, Gabor; Valyi-Nagy, Istvan; Orfi, Laszlo; Ullrich, Axel; Csala, Miklos; Keri, Gyorgy

doi:10.1016/j.bmcl.2015.11.099

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Novel compounds reducing IRS-1 serine phosphorylation for treatment of diabetes

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Ullrich, Axel
Ullrich, Axel / Molecular Biology, Max Planck Institute of Biochemistry, Max Planck Society;

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引用

Simon-Szabo, L., Kokas, M., Greff, Z., Boros, S., Banhegyi, P., Zsakai, L., Szantai-Kis, C., Vantus, T., Mandl, J., Banhegyi, G., Valyi-Nagy, I., Orfi, L., Ullrich, A., Csala, M., & Keri, G. (2016). Novel compounds reducing IRS-1 serine phosphorylation for treatment of diabetes. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 26(2), 424-428. doi:10.1016/j.bmcl.2015.11.099.

引用: https://hdl.handle.net/11858/00-001M-0000-0029-C8FA-1

要旨

Activation of various interacting stress kinases, particularly the c-Jun N-terminal kinases (JNK), and a concomitant phosphorylation of insulin receptor substrate 1 (IRS-1) at serine 307 play a central role both in insulin resistance and in beta-cell dysfunction. IRS-1 phosphorylation is stimulated by elevated free fatty acid levels through different pathways in obesity. A series of novel pyrido[2,3-d]pyrimidin-7-one derivatives were synthesized as potential antidiabetic agents, preventing IRS-1 phosphorylation at serine 307 in a cellular model of lipotoxicity and type 2 diabetes. (C) 2015 Elsevier Ltd. All rights reserved.