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Mini-Review Article

70 kDa核糖体蛋白S6激酶(P70S6K)抑制剂作为治疗肥胖、2型糖尿病和癌症的有效工具的研究进展

卷 27, 期 28, 2020

页: [4699 - 4719] 页: 21

弟呕挨: 10.2174/0929867327666200114113139

价格: $65

摘要

目前 ,如肥胖、Ⅱ型糖尿病和癌症等疾病带来的严重健康问题与mTOR通路密切相关。70 kDa核糖体蛋白S6激酶(p70S6K)是mTOR的重要下游效应因子，介导蛋白合成、RNA加工、葡萄糖稳态、细胞生长和凋亡。抑制p70S6K的功能可以降低肥胖的风险，有助于治疗血脂异常，提高胰岛素敏感性，延长哺乳动物的寿命。因此，p70S6K成为治疗这些疾病的潜在靶点。目前，除了辉瑞公司开发的第一个p70S6K特异性抑制剂PF-4708671和礼来公司开发的LY2584702外，所有p70S6K抑制剂均处于临床前研究阶段。本文简要介绍了p70S6K的概况，并对其近年来的抑制剂进行了综述，主要将其分为两类:天然化合物和合成化合物。特别强调了它们的抑制活性、构效关系(SARs)和机制。

关键词: p70S6K，潜在靶标、疾病、抑制剂、活性、构效关系。

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