摘要
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.
出处
《中南药学》
CAS
2017年第11期1555-1562,共8页
Central South Pharmacy
基金
国家自然科学基金项目(No.81660570)
现代药物研究开发协同创新中心(黔教合协同创新字[2013]04)
贵州省民族药药效物质基础研究科技创新人才团队\贵州省高层次创新型人才培养(百层次)(黔科合平台人才[2016]5613\5677)