Department of Oncology, The Sidney Kimmel Comprehensive Cancer Center, Johns Hopkins University, Baltimore, MD 21231, USA.
Mol Cancer Res. 2011 Dec;9(12):1746-54. doi: 10.1158/1541-7786.MCR-11-0286. Epub 2011 Oct 12.
The Notch signaling pathway is a critical embryonic developmental regulatory pathway that has been implicated in oncogenesis. In non-small cell lung cancer (NSCLC), recent evidence suggests that Notch signaling may contribute to maintenance of a cancer stem or progenitor cell compartment required for tumorigenesis. We explored whether intact Notch signaling is required for NSCLC clonogenic and tumorigenic potential in vitro and in vivo using a series of genetically modified model systems. In keeping with previous observations, we find that Notch3 in particular is upregulated in human lung cancer lines and that downregulation of Notch signaling using a selective γ-secretase inhibitor (MRK-003) is associated with decreased proliferation and clonogenic capacity in vitro. We show that this phenotype is rescued with the expression of NICD3, a constitutively active cleaved form of Notch3 not affected by γ-secretase inhibition. Using an inducible LSL-KRAS(G12D) model of lung cancer in vivo, we show a transient upregulation of Notch pathway activity in early tumor precursor lesions. However, a more rigorous test of the requirement for Notch signaling in lung oncogenesis, crossing the LSL-KRAS(G12D) mouse model with a transgenic with a similarly inducible global dominant-negative suppressor of Notch activity, LSL-DNMAML (dominant-negative mastermind-like), reveals no evidence of Notch pathway requirement for lung tumor initiation or growth in vivo. Distinct Notch family members may have different and potentially opposing activities in oncogenesis, and targeted inhibition of individual Notch family members may be a more effective anticancer strategy than global pathway suppression.
Notch 信号通路是一种关键的胚胎发育调控通路,已被牵涉到肿瘤发生中。在非小细胞肺癌(NSCLC)中,最近的证据表明 Notch 信号可能有助于维持肿瘤发生所需的癌症干细胞或祖细胞区室。我们使用一系列基因修饰模型系统,探讨了 Notch 信号通路在 NSCLC 克隆形成和致瘤性的体外和体内是否完整。与以前的观察结果一致,我们发现 Notch3 特别是在人类肺癌系中上调,并且使用选择性 γ-分泌酶抑制剂(MRK-003)下调 Notch 信号与体外增殖和克隆形成能力下降有关。我们表明,这种表型可以通过 NICD3 的表达得到挽救,NICD3 是 Notch3 的一种组成性激活的切割形式,不受 γ-分泌酶抑制的影响。我们使用体内 LSL-KRAS(G12D)肺癌模型,显示 Notch 通路活性在早期肿瘤前病变中短暂上调。然而,对 Notch 信号在肺癌发生中的必要性进行更严格的测试,即与一种可诱导的全局显性负性 Notch 活性抑制剂 LSL-DNMAML(显性负性 mastermind-like)的转基因小鼠模型交叉,并没有发现 Notch 通路在体内肺肿瘤起始或生长中的必要性的证据。不同的 Notch 家族成员在肿瘤发生中可能具有不同的和潜在的相反的活性,并且针对单个 Notch 家族成员的靶向抑制可能比全局通路抑制更有效抗癌策略。