449811-76-1Relevant academic research and scientific papers
Novel compounds reducing IRS-1 serine phosphorylation for treatment of diabetes
Simon-Szabó, Laura,Kokas, Márton,Greff, Zoltán,Boros, Sándor,Bánhegyi, Péter,Zsákai, Lilián,Szántai-Kis, Csaba,Vantus, Tibor,Mandl, József,Bánhegyi, Gábor,Vályi-Nagy, István,Orfi, László,Ullrich, Axel,Csala, Miklós,Kéri, Gy?rgy
, p. 424 - 428 (2016)
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 β-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.
