Departments of Respiratory Medicine and Allergology, Research Institute for Frontier Medicine, Sapporo Medical University School of Medicine, Sapporo, Japan.
Departments of Biochemistry, Research Institute for Frontier Medicine, Sapporo Medical University School of Medicine, Sapporo, Japan.
Oncogene. 2017 Nov 16;36(46):6432-6445. doi: 10.1038/onc.2017.253. Epub 2017 Jul 24.
Tyrosine kinase inhibitor (TKI)-sensitive and TKI-resistant mutations of epidermal growth factor receptor (EGFR) are associated with lung adenocarcinoma. EGFR mutants were previously shown to exhibit ligand-independent activation. We have previously demonstrated that pulmonary surfactant protein D (SP-D, SFTPD) suppressed wild-type EGFR signaling by blocking ligand binding to EGFR. We herein demonstrate that SFTPD downregulates ligand-independent signaling in cells harboring EGFR mutations such as TKI-sensitive exon 19 deletion (Ex19del) and L858R mutation as well as TKI-resistant T790M mutation, subsequently suppressing cellular growth and motility. Lectin blotting and ligand blotting in lung cancer cell lines suggested that EGFR mutants express oligomannose-type N-glycans and interact with SFTPD directly. Cross-linking assay indicated that SFTPD inhibits ligand-independent dimerization of EGFR mutants. We also demonstrated that SFTPD reduced dimerization-independent phosphorylation of Ex19del and T790M EGFR mutants using point mutations that disrupted the asymmetric dimer interface. It was confirmed that SFTPD augmented the viability-suppressing effects of EGFR-TKIs. Furthermore, retrospective analysis of 121 patients with lung adenocarcinoma to examine associations between serum SFTPD levels and clinical outcome indicated that in TKI-treated patients with lung cancer harboring EGFR mutations, including Ex19del or L858R, high serum SFTPD levels correlated with a lower number of distant metastases and prolonged overall survival and progression-free survival. These findings suggest that SFTPD downregulates both TKI-sensitive and -resistant EGFR mutant signaling, and SFTPD level is correlated with clinical outcome. These findings illustrate the use of serum SFTPD level as a potential marker to estimate the efficacy of EGFR-TKIs.
表皮生长因子受体 (EGFR) 的酪氨酸激酶抑制剂 (TKI)-敏感和 TKI-耐药突变与肺腺癌有关。先前已经表明,EGFR 突变体表现出配体非依赖性激活。我们之前已经证明,肺表面活性蛋白 D (SP-D,SFTPD) 通过阻止配体与 EGFR 结合来抑制野生型 EGFR 信号。我们在此证明 SFTPD 下调了携带 EGFR 突变的细胞中的配体非依赖性信号,例如 TKI 敏感的外显子 19 缺失 (Ex19del) 和 L858R 突变以及 TKI 耐药的 T790M 突变,从而抑制细胞生长和迁移。肺癌细胞系中的凝集素印迹和配体印迹表明,EGFR 突变体表达寡甘露糖型 N-糖基,并与 SFTPD 直接相互作用。交联实验表明 SFTPD 抑制 EGFR 突变体的配体非依赖性二聚化。我们还证明 SFTPD 通过破坏不对称二聚体界面的点突变来减少 Ex19del 和 T790M EGFR 突变体的二聚化非依赖性磷酸化。证实 SFTPD 增强了 EGFR-TKIs 的抑制细胞活力的作用。此外,对 121 例肺腺癌患者进行的回顾性分析,以检查血清 SFTPD 水平与临床结果之间的关系,表明在携带 EGFR 突变(包括 Ex19del 或 L858R)的肺癌患者中,TKI 治疗后,血清 SFTPD 水平高与远处转移数量减少、总生存期和无进展生存期延长相关。这些发现表明 SFTPD 下调了 TKI 敏感和耐药的 EGFR 突变体信号,并且 SFTPD 水平与临床结果相关。这些发现说明了血清 SFTPD 水平作为一种潜在的标志物来评估 EGFR-TKIs 的疗效。