Department of Applied Chemistry, Faculty of Science and Technology, Keio University, Yokohama, Japan.
Cancer Sci. 2022 Mar;113(3):950-959. doi: 10.1111/cas.15258. Epub 2022 Jan 12.
ErbB4 is a member of the ErbB receptor tyrosine kinase family. It has both pro- and anti-oncogenic activities in tumors. Vasculogenic mimicry (VM), a phenomenon in which cancer cells form capillary-like structures without endothelial cells, has been recognized to be a cause of malignant phenotypes in some solid tumors. Here, we used an in vitro VM formation assay, and demonstrated that ErbB4 negatively regulated VM formation in human breast cancer cells. By using CRISPR/Cas9-mediated gene knockout, we verified that the depletion of endogenous ErbB4 improved the VM formation capability. Although treatment with neuregulin 1 (NRG1), a ligand of ErbB4, induced the phosphorylation of ErbB4 and promoted VM formation in a dose-dependent manner, it did not induce such activities in kinase-dead K751M ErbB4-overexpressing cells. Moreover, we examined the effect of the missense mutation E872K of ErbB4, which has been reported in multiple tumors, on VM formation, and found that the mutation enhanced the basal phosphorylation level and ErbB4-mediated VM formation in the absence of NRG1 stimulation. Whereas NRG1 stimulated VM formation, excessive activation of ErbB4 induced a negative effect. In E872K ErbB4-overexpressing cells, but not in wild-type ErbB4-overexpressing cells, the number of VM tubes was significantly decreased by low-dose treatment with the ErbB inhibitor afatinib. Taken together, our findings demonstrated the significance of ErbB4-mediated VM formation, and suggested the possibility of ErbB4 mutations as effective targets in breast cancer.
ErbB4 是 ErbB 受体酪氨酸激酶家族的一员。它在肿瘤中既有原癌基因又有抑癌基因的活性。血管生成拟态(VM)是一种癌细胞在没有内皮细胞的情况下形成类似毛细血管的结构的现象,已被认为是某些实体瘤恶性表型的原因。在这里,我们使用了体外 VM 形成测定法,并证明 ErbB4 负调控人乳腺癌细胞中的 VM 形成。通过使用 CRISPR/Cas9 介导的基因敲除,我们验证了内源性 ErbB4 的耗竭改善了 VM 形成能力。虽然用 ErbB4 的配体神经调节蛋白 1(NRG1)处理以剂量依赖性方式诱导 ErbB4 的磷酸化并促进 VM 形成,但它不会诱导激酶失活的 K751M ErbB4 过表达细胞中的这种活性。此外,我们检查了已在多种肿瘤中报道的 ErbB4 的错义突变 E872K 对 VM 形成的影响,发现该突变增强了基础磷酸化水平和无 NRG1 刺激时 ErbB4 介导的 VM 形成。虽然 NRG1 刺激 VM 形成,但 ErbB4 的过度激活诱导了负效应。在没有 NRG1 刺激的情况下,E872K ErbB4 过表达细胞中,而不是在野生型 ErbB4 过表达细胞中,用 ErbB 抑制剂 afatinib 进行低剂量处理显著减少了 VM 管的数量。总之,我们的研究结果表明 ErbB4 介导的 VM 形成的重要性,并提出 ErbB4 突变作为乳腺癌有效靶点的可能性。