Provenzano Paolo P, Inman David R, Eliceiri Kevin W, Beggs Hilary E, Keely Patricia J
Department of Pharmacology, Laboratory of Molecular Biology, Madison, WI 53706, USA. ppproven@ wisc.edu
Am J Pathol. 2008 Nov;173(5):1551-65. doi: 10.2353/ajpath.2008.080308. Epub 2008 Oct 9.
Focal adhesion kinase (FAK) is a central regulator of the focal adhesion, influencing cell proliferation, survival, and migration. Despite evidence demonstrating FAK overexpression in human cancer, its role in tumor initiation and progression is not well understood. Using Cre/LoxP technology to specifically knockout FAK in the mammary epithelium, we showed that FAK is not required for tumor initiation but is required for tumor progression. The mechanistic underpinnings of these results suggested that FAK regulates clinically relevant gene signatures and multiple signaling complexes associated with tumor progression and metastasis, such as Src, ERK, and p130Cas. Furthermore, a systems-level analysis identified FAK as a major regulator of the tumor transcriptome, influencing genes associated with adhesion and growth factor signaling pathways, and their cross talk. Additionally, FAK was shown to down-regulate the expression of clinically relevant proliferation- and metastasis-associated gene signatures, as well as an enriched group of genes associated with the G(2) and G(2)/M phases of the cell cycle. Computational analysis of transcription factor-binding sites within ontology-enriched or clustered gene sets suggested that the differentially expressed proliferation- and metastasis-associated genes in FAK-null cells were regulated through a common set of transcription factors, including p53. Therefore, FAK acts as a primary node in the activated signaling network in transformed motile cells and is a prime candidate for novel therapeutic interventions to treat aggressive human breast cancers.
粘着斑激酶(FAK)是粘着斑的核心调节因子,影响细胞增殖、存活和迁移。尽管有证据表明FAK在人类癌症中过表达,但其在肿瘤发生和进展中的作用尚未完全了解。利用Cre/LoxP技术在乳腺上皮细胞中特异性敲除FAK,我们发现FAK不是肿瘤发生所必需的,但却是肿瘤进展所必需的。这些结果的机制基础表明,FAK调节与肿瘤进展和转移相关的临床相关基因特征和多种信号复合物,如Src、ERK和p130Cas。此外,系统水平分析确定FAK是肿瘤转录组的主要调节因子,影响与粘附和生长因子信号通路相关的基因及其相互作用。此外,FAK被证明可下调与临床相关的增殖和转移相关基因特征的表达,以及一组与细胞周期G(2)和G(2)/M期相关的富集基因。对本体富集或聚类基因集中转录因子结合位点的计算分析表明,FAK缺失细胞中差异表达的增殖和转移相关基因是通过一组共同的转录因子调节的,包括p53。因此,FAK在转化的运动细胞中作为激活信号网络的主要节点,是治疗侵袭性人类乳腺癌的新型治疗干预的主要候选者。