State Key Laboratory of Oncogenes and Related Genes, Renji Hospital, Shanghai Jiaotong University School of Medicine, Shanghai Cancer Institute.
Neoplasia. 2011 May;13(5):461-71. doi: 10.1593/neo.101744.
Several types of epidermal growth factor receptor (EGFR) gene alternations have been observed in human tumors. Here we present a novel EGFR variant with aberrant splicing of exon 4 (named as de4 EGFR). Variant-specific polymerase chain reaction showed that de4 EGFR was expressed in some glioma (4/40), prostate cancer (3/11), and ovarian cancer (3/9) tissues but not in tissues adjacent to tumors or normal tissues. de4 EGFR displayed an enhanced transformation and a higher metastasis-promoting capacity in comparison to wild-type EGFR. With minimal EGF-binding activity, de4 EGFR underwent ligand-independent autophosphorylation and self-dimerization. Moreover, in serum-starved condition, de4 EGFR expression in U87 MG cells significantly upregulated the extracellular signal-regulated kinase and AKT phosphorylation and expression of JUN and Src. Importantly, E-cadherin expression was barely detectable in the U87 MG cells expressing de4 EGFR and restored expression of E-cadherin in these cells inhibited their metastatic behaviors. Taken together, we identified a novel EGFR variant with increased metastasis-promoting activity that may become a promising new target for cancer therapy.
已在人类肿瘤中观察到几种表皮生长因子受体 (EGFR) 基因改变。在这里,我们提出了一种新的 EGFR 变体,其外显子 4 发生异常剪接(命名为 de4 EGFR)。变体特异性聚合酶链反应显示,de4 EGFR 在一些脑胶质瘤(4/40)、前列腺癌(3/11)和卵巢癌(3/9)组织中表达,但在肿瘤相邻组织或正常组织中不表达。与野生型 EGFR 相比,de4 EGFR 表现出增强的转化和更高的促进转移能力。de4 EGFR 与 EGF 的结合活性最小,但能进行配体非依赖性的自身磷酸化和自身二聚化。此外,在血清饥饿条件下,U87 MG 细胞中 de4 EGFR 的表达显著上调了细胞外信号调节激酶和 AKT 的磷酸化以及 JUN 和 Src 的表达。重要的是,在表达 de4 EGFR 的 U87 MG 细胞中几乎检测不到 E-钙黏蛋白的表达,而这些细胞中 E-钙黏蛋白的恢复表达抑制了它们的转移行为。总之,我们鉴定出一种具有增强转移促进活性的新型 EGFR 变体,它可能成为癌症治疗的一个有前途的新靶点。