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Review Article

STAT3抑制剂的发现：近期进展和未来展望

卷 30, 期 16, 2023

发表于: 04 October, 2022

页: [1824 - 1847] 页: 24

弟呕挨: 10.2174/0929867329666220819093117

价格: $65

摘要

背景：STAT3（信号转导子和转录激活子3）是STAT家族蛋白的一员，起信号转导子及转录因子的作用。先前的研究已经证明了它在细胞增殖、分化、凋亡以及免疫和炎症反应中的重要性。靶向STAT3蛋白最近被誉为一种可行的癌症治疗方法。尽管这些抑制剂中没有一种在临床癌症治疗中得到开发，但有一小部分已经进入临床试验，这导致研究人员探索更有前景的抑制剂。 方法：从STAT3激活机制出发，根据STAT3抑制剂的来源、结构、生物活性和作用机制，对几种类型的STAT3抑制剂进行了描述和总结。STAT3的直接抑制主要针对蛋白质的三个不同结构区域之一，即SH2结构域、DNA结合结构域和螺旋线圈结构域。 结果：综述了2010年至2021 STAT3抑制剂发现的进展。STAT3抑制剂主要分为小分子抑制剂、天然产物抑制剂和肽/肽抑制剂。此外，它还涵盖了相关的类似物及其核心框架。 结论：STAT3小分子抑制剂如BP-1-102和BTP类似物对各种癌症显示出巨大的潜力，而天然产物以及肽和肽模拟物也显示出有前景的应用。因此，STAT3已成为极具研究价值的靶点，STAT3抑制剂的开发可能为STAT3相关疾病提供更多的治疗策略。

关键词: STAT3（信号转导和转录激活因子3），结构域，小分子抑制剂，天然产物，抗癌治疗，细胞增殖。

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