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首页> 外文期刊>ACS Omega >Novel Sulfonanilide Inhibitors of SHIP2 Enhance Glucose Uptake into Cultured Myotubes
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Novel Sulfonanilide Inhibitors of SHIP2 Enhance Glucose Uptake into Cultured Myotubes

机译：船舶2的新型磺胺苯胺抑制剂增强葡萄糖摄取到培养的肌管中

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摘要

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.
机译：制备了一系列取代的磺硅烷类似物，并评价为含SH2结构域的肌醇多磷酸5'-磷酸酶2的新型有效抑制剂（Ship2）。 Ship2已被证明是一种新的糖尿病（T2D）治疗胰岛素抵抗的新诱人目标，这可能导致危及生命的糖尿病肾病（DKD）。在合成化合物中，两个最有前途的候选物，10和11，显着抑制了舰船。另外，这些化合物以剂量依赖性方式诱导AKT活化，增加葡萄糖转运蛋白4在质膜上的存在，并在较低浓度的体外增强葡萄糖摄取比二甲双胍，最广泛使用的抗糖尿病药物。这些结果表明，新型船舶2抑制剂具有胰岛素敏感性，为T2D和DKD提供了进一步的药物开发的原型。

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