van Nimwegen Maroesja J, van de Water Bob
Division of Toxicology, Leiden/Amsterdam Center for Drug Research, Leiden University, Gorlaeus Laboratories, 2300 RA Leiden, The Netherlands.
Biochem Pharmacol. 2007 Mar 1;73(5):597-609. doi: 10.1016/j.bcp.2006.08.011. Epub 2006 Sep 25.
Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase that plays an important role in signal transduction pathways that are initiated at sites of integrin-mediated cell adhesions and by growth factor receptors. FAK is a key regulator of survival, proliferation, migration and invasion: processes that are all involved in the development and progression of cancer. FAK is also linked to oncogenes at both a biochemical and functional level. Moreover, overexpression and/or increased activity of FAK is common in a wide variety of human cancers, implicating a role for FAK in carcinogenesis. Given the important role of FAK in a large number of processes involved in tumorigenesis, metastasis and survival signalling FAK should be regarded as a potential target in the development of anti-cancer drugs. Therefore, selective inhibitors of FAK need to be developed. Combination of these selective FAK inhibitors with cytotoxic agents could be a very promising anti-cancer therapy.
粘着斑激酶（FAK）是一种非受体酪氨酸激酶，在由整合素介导的细胞粘附位点以及生长因子受体启动的信号转导途径中发挥重要作用。FAK是存活、增殖、迁移和侵袭的关键调节因子，而这些过程均参与癌症的发生和发展。FAK在生化和功能水平上也与癌基因相关联。此外，FAK的过表达和/或活性增加在多种人类癌症中很常见，这表明FAK在致癌过程中发挥作用。鉴于FAK在肿瘤发生、转移和存活信号传导的大量过程中具有重要作用，FAK应被视为抗癌药物开发中的潜在靶点。因此，需要开发FAK的选择性抑制剂。将这些选择性FAK抑制剂与细胞毒性药物联合使用可能是一种非常有前景的抗癌疗法。
