Division of Pulmonary Critical Care Medicine, Department of Internal Medicine, Kaohsiung Medical University Hospital, Kaohsiung Medical University, Kaohsiung 80708, Taiwan.
Division of Nephrology, Department of Internal Medicine, Kaohsiung Medical University Hospital, Kaohsiung Medical University, Kaohsiung 80708, Taiwan.
Int J Mol Sci. 2022 Feb 2;23(3):1726. doi: 10.3390/ijms23031726.
Focal adhesion kinase (FAK), a non-receptor tyrosine kinase, is overexpressed and activated in many cancer types. FAK regulates diverse cellular processes, including growth factor signaling, cell cycle progression, cell survival, cell motility, angiogenesis, and the establishment of immunosuppressive tumor microenvironments through kinase-dependent and kinase-independent scaffolding functions in the cytoplasm and nucleus. Mounting evidence has indicated that targeting FAK, either alone or in combination with other agents, may represent a promising therapeutic strategy for various cancers. In this review, we summarize the mechanisms underlying FAK-mediated signaling networks during tumor development. We also summarize the recent progress of FAK-targeted small-molecule compounds for anticancer activity from preclinical and clinical evidence.
黏着斑激酶（FAK）是一种非受体酪氨酸激酶，在许多癌症类型中过表达和激活。FAK 通过在细胞质和核内的激酶依赖和激酶非依赖的支架功能调节多种细胞过程，包括生长因子信号转导、细胞周期进程、细胞存活、细胞迁移、血管生成以及建立免疫抑制性肿瘤微环境。越来越多的证据表明，单独或联合其他药物靶向 FAK 可能代表了各种癌症有前途的治疗策略。在这篇综述中，我们总结了 FAK 介导的信号网络在肿瘤发展过程中的作用机制。我们还总结了近年来基于临床前和临床证据的靶向 FAK 的小分子化合物在抗癌活性方面的最新进展。
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