Institute of Pharmacology and Toxicology, Rostock University Medical Center, Schillingallee 70, 18057 Rostock, Germany.
Int J Mol Sci. 2021 Jun 21;22(12):6606. doi: 10.3390/ijms22126606.
Tissue factor (TF) plays an important role in the progression and angiogenesis of tumor cells. The present study investigated the mechanism of interleukin-1β (IL-1β)-induced TF expression in A549 lung cancer cells. Based on mRNA and protein analyses, including appropriate inhibitor experiments, IL-1β was shown to induce TF expression in a time-dependent manner, mediated by IL-1 receptor-dependent phosphorylation of the mitogen-activated protein kinases (MAPK) p38, p42/44 and c-jun N-terminal kinase (JNK), as well as the Src kinase and the epidermal growth factor receptor (EGFR). Thereby, inhibition of EGFR transactivation by the Src inhibitor PP1 or direct EGFR inhibition by the EGFR tyrosine kinase inhibitor (TKI) erlotinib led to a reduction of IL-1β-induced TF expression and to a suppression of p42/44 MAPK and EGFR activation, while IL-1β-induced p38 MAPK and JNK activation remained unchanged. A knockdown of EGFR by siRNA was associated with decreased IL-1β-mediated p42/44 MAPK activation, which was no longer inhibitable by erlotinib. Concentration-dependent inhibition of IL-1β-induced TF expression was also observed in the presence of gefitinib and afatinib, two other EGFR TKIs. In summary, our results suggest that IL-1β leads to increased TF formation in lung cancer cells via both Src/EGFR/p42/44 MAPK-dependent and EGFR-independent signaling pathways, with the latter mediated via p38 MAPK and JNK.
组织因子 (TF) 在肿瘤细胞的进展和血管生成中发挥重要作用。本研究探讨了白细胞介素-1β (IL-1β) 诱导 A549 肺癌细胞 TF 表达的机制。基于 mRNA 和蛋白质分析,包括适当的抑制剂实验,表明 IL-1β以时间依赖性方式诱导 TF 表达,由 IL-1 受体依赖性丝裂原活化蛋白激酶 (MAPK) p38、p42/44 和 c-jun N 末端激酶 (JNK) 的磷酸化以及Src 激酶和表皮生长因子受体 (EGFR) 介导。因此,Src 抑制剂 PP1 抑制 EGFR 转激活或 EGFR 酪氨酸激酶抑制剂 (TKI) 厄洛替尼直接抑制 EGFR,导致 IL-1β诱导的 TF 表达减少,并抑制 p42/44 MAPK 和 EGFR 激活,而 IL-1β诱导的 p38 MAPK 和 JNK 激活保持不变。通过 siRNA 敲低 EGFR 与 IL-1β 介导的 p42/44 MAPK 激活减少有关,而厄洛替尼不再抑制该激活。在存在吉非替尼和阿法替尼两种其他 EGFR TKI 的情况下,也观察到 IL-1β 诱导的 TF 表达呈浓度依赖性抑制。总之,我们的结果表明,IL-1β 通过 Src/EGFR/p42/44 MAPK 依赖性和 EGFR 非依赖性信号通路导致肺癌细胞中 TF 形成增加,后者通过 p38 MAPK 和 JNK 介导。