Deng Xu-Bin, Xiao Li, Wu Yue, Jin Fang, Mossman Brooke, Testa Joseph R, Xiao Guang-Hui
Cancer Institute, Southern Medical University, Guangzhou, China.
Cancer Biology Program, Fox Chase Cancer Center, Philadelphia, PA.
Int J Cancer. 2015 Jul 15;137(2):481-90. doi: 10.1002/ijc.29391. Epub 2014 Dec 27.
Malignant mesothelioma (MM) is a highly invasive and chemoresistant malignancy induced by asbestos fibers. NK4, a hepatocyte growth factor antagonist and angiogenesis inhibitor, consists of the N-terminal hairpin domain and four kringle domains of the α-chain of hepatocyte growth factor. The therapeutic potential of NK4 has been demonstrated in a variety of tumor types. However, the mechanisms by which NK4 inhibits tumor growth have not been well delineated. In this study, it is shown that the NK4 adenovirus (Ad-NK4) potently inhibits cell viability, invasiveness and tumorigenicity of human MM cells. Significantly, this study demonstrates for the first time that Ad-NK4 inhibits cancer stem-like cell (CSC) properties as assessed by spheroid formation assay, side population analysis and flow cytometric sorting of CD24 cells. In addition to inhibiting phosphorylation of Met and AKT, Ad-NK4 markedly suppressed the active form of β-catenin, a key mediator of both Wnt and AKT pathways. It is further demonstrated that expression of NK4 suppresses β-catenin nuclear localization and transcriptional activity. Intriguingly, the expression levels of Oct4 and Myc, two critical stem cell factors and downstream targets of β-catenin, were also diminished by Ad-NK4. Furthermore, the strong antitumor effect of NK4 was found to be linked to its ability to inhibit CSCs as revealed by immunohistochemical examination of tumor specimens from a mouse xenograft model of human MM. These findings suggest that NK4 acts as a CSC inhibitor by impeding Met/AKT/β-catenin signaling and holds promise for achieving durable therapeutic responses in MM by constraining the CSC component of these aggressive tumors.
恶性间皮瘤(MM)是一种由石棉纤维诱导产生的具有高度侵袭性和化学抗性的恶性肿瘤。NK4是一种肝细胞生长因子拮抗剂和血管生成抑制剂,由肝细胞生长因子α链的N端发夹结构域和四个kringle结构域组成。NK4在多种肿瘤类型中的治疗潜力已得到证实。然而,NK4抑制肿瘤生长的机制尚未完全阐明。在本研究中,结果表明NK4腺病毒(Ad-NK4)能有效抑制人MM细胞的细胞活力、侵袭性和致瘤性。重要的是,本研究首次证明,通过球体形成试验、侧群分析和CD24细胞的流式细胞术分选评估,Ad-NK4可抑制癌症干细胞样细胞(CSC)特性。除了抑制Met和AKT的磷酸化外,Ad-NK4还显著抑制了β-连环蛋白的活性形式,β-连环蛋白是Wnt和AKT通路的关键介质。进一步证明,NK4的表达抑制了β-连环蛋白的核定位和转录活性。有趣的是,Ad-NK4还降低了Oct4和Myc这两个关键干细胞因子以及β-连环蛋白下游靶点的表达水平。此外,通过对人MM小鼠异种移植模型的肿瘤标本进行免疫组化检查发现,NK4的强大抗肿瘤作用与其抑制CSC的能力有关。这些发现表明,NK4通过阻碍Met/AKT/β-连环蛋白信号传导发挥CSC抑制剂的作用,并有望通过抑制这些侵袭性肿瘤的CSC成分在MM中实现持久的治疗反应。