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General Review Article

信号转导和转录蛋白3（STAT3）的激活剂：作为有希望的抗癌药的直接抑制剂的更新。

卷 26, 期 27, 2019

页: [5165 - 5206] 页: 42

弟呕挨: 10.2174/0929867325666180719122729

价格: $65

摘要

背景：由于信号转导子和转录激活因子3（STAT3）是一种转录因子，在癌症的各个方面（包括疾病的进展和迁移）中都起着重要的作用，并且在各种人类肿瘤中都被组成性激活，因此已证实STAT3的抑制作用已得到验证。几种恶性肿瘤的治疗策略。这篇综述的目的是提供有关靶向STAT3结构域的新有希望的直接抑制剂作为潜在抗癌药的鉴定的最新信息。 方法：针对最近报道的STAT3直接抑制剂进行了全面的文献检索。我们考虑了有关STAT3域的相关进展，这些已被确定为潜在的药物靶标。 结果：详细引用了135篇经同行评审的论文和7项专利；我们考虑的抑制剂靶向DNA结合域（化合物分为天然衍生物，小分子，肽，适体和寡核苷酸），SH2结合域（天然，半合成和合成化合物）和特定的残基，例如半胱氨酸（天然，半合成，合成化合物和双重抑制剂）和酪氨酸705。 结论：尽管目前尚无靶向这种酶的药物可用于抗癌治疗，但最近鉴定出的大量直接STAT3抑制剂显示出对这一靶标研究的浓厚兴趣，尽管这是一项艰巨的任务。值得注意的是，对可用抑制剂的许多研究表明它们中的一些具有双重作用机理。

关键词: STAT3直接抑制，SH2结构域，DNA结合结构域，半胱氨酸，小分子，天然化合物，半合成化合物。

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