局部黏着斑激酶抑制剂的研究进展

Research progress in focal adhesion kinase inhibitors

局部黏着斑激酶(focal adhesion kinase,FAK)是一种非受体酪氨酸激酶,其作为整合素介导信号传导过程中的关键分子参与肿瘤多个信号通路的调节,与肿瘤细胞增殖、迁移、侵袭、凋亡及血管生成等密切相关。设计高选择性的FAK抑制剂阻断或调控由FAK介导的肿瘤是目前抗肿瘤药物开发的重要方向。近年来大量结构新颖的FAK抑制剂被相继报道,因此,本文将对其进行总结,为新型抗肿瘤药物的开发提供参考。

Focal adhesion kinase （FAK） is a non-receptor tyrosine kinase. As a key molecule of the signal transduction mediated by integrin, FAK is involved in multiple signaling pathways of tumor regulation, such as the proliferation, migration, invasion, apoptosis and angiogenesis. To design of highly selective inhibitors of FAK is important for the development of novel antitumor drugs. In recent years, a large number of novel FAK inhibitors have been reported, and this article will summarize these compounds for the development of new antitumor agents.