Chuang Hsiang-Hao, Huang Ming-Shyan, Zhen Yen-Yi, Chuang Cheng-Hao, Lee Ying-Ray, Hsiao Michael, Yang Chih-Jen
Division of Pulmonary Critical Care Medicine, Department of Internal Medicine, Kaohsiung Medical University Hospital, Kaohsiung Medical University, Kaohsiung 80708, Taiwan.
Department of Internal Medicine, E-Da Cancer Hospital, School of Medicine, I-Shou University, Kaohsiung 82445, Taiwan.
Biomedicines. 2022 Aug 10;10(8):1937. doi: 10.3390/biomedicines10081937.
Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase overexpressed in various cancer types that plays a critical role in tumor progression. Accumulating evidence suggests that targeting FAK, either alone or in combination with other agents, may serve as an effective therapeutic strategy for numerous cancers. In addition to retarding proliferation, metastasis, and angiogenesis, FAK inhibition triggers cellular senescence in lung cancer cells. However, the detailed mechanism remains enigmatic. In the present study, we found that FAK inhibition not only elicits DNA-damage signaling but also downregulates enhancer of zeste homolog 2 (EZH2) expression. The manipulation of FAK expression influences EZH2 expression and corresponding signaling in vitro. Immunohistochemistry shows that active FAK signaling corresponds with the activation of the EZH2-mediated signaling cascade in lung-cancer-cells-derived tumor tissues. We also found that ectopic EZH2 expression attenuates FAK-inhibition-induced cellular senescence in lung cancer cells. Our results identify EZH2 as a critical downstream effector of the FAK-mediated anti-senescence pathway. Targeting FAK-EZH2 axis-induced cellular senescence may represent a promising therapeutic strategy for restraining tumor growth.
粘着斑激酶(FAK)是一种非受体酪氨酸激酶,在多种癌症类型中过表达,在肿瘤进展中起关键作用。越来越多的证据表明,单独或与其他药物联合靶向FAK,可能成为治疗多种癌症的有效策略。除了抑制增殖、转移和血管生成外,FAK抑制还能触发肺癌细胞的细胞衰老。然而,具体机制仍不清楚。在本研究中,我们发现FAK抑制不仅引发DNA损伤信号,还下调zeste同源物2(EZH2)增强子的表达。在体外,FAK表达的调控影响EZH2表达及相应信号。免疫组织化学显示,在肺癌细胞来源的肿瘤组织中,活跃的FAK信号与EZH2介导的信号级联激活相对应。我们还发现,异位表达EZH2可减弱FAK抑制诱导的肺癌细胞衰老。我们的结果表明EZH2是FAK介导的抗衰老途径的关键下游效应物。靶向FAK-EZH2轴诱导的细胞衰老可能是抑制肿瘤生长的一种有前景的治疗策略。