Wells Center for Pediatric Research, Departments of Pediatrics, Biochemistry/Molecular Biology and Pharmacology/ Toxicology, The Simon Cancer Center, Indiana University School of Medicine, Indianapolis, Indiana 46074, USA.
J Biol Chem. 2012 Nov 2;287(45):38356-66. doi: 10.1074/jbc.M112.377382. Epub 2012 Sep 19.
Activation of the Hedgehog (Hh) pathway is known to drive development of basal cell carcinoma and medulloblastomas and to associate with many other types of cancer, but the exact molecular mechanisms underlying the carcinogenesis process remain elusive. We discovered that skin tumors derived from epidermal expression of oncogenic Smo, SmoM2, have elevated levels of IL-11, IL-11Rα, and STAT3 phosphorylation at Tyr(705). The relevance of our data to human conditions was reflected by the fact that all human basal cell carcinomas examined have detectable STAT3 phosphorylation, mostly in keratinocytes. The functional relevance of STAT3 in Smo-mediated carcinogenesis was revealed by epidermal specific knockout of STAT3. We showed that removal of STAT3 from mouse epidermis dramatically reduced SmoM2-mediated cell proliferation, leading to a significant decrease in epidermal thickness and tumor development. We also observed a significant reduction of epidermal stem/progenitor cell population and cyclin D1 expression in mice with epidermis-specific knockout of STAT3. Our evidence indicates that STAT3 signaling activation may be mediated by the IL-11/IL-11Rα signaling axis. We showed that tumor development was reduced after induced expression of SmoM2 in IL-11Rα null mice. Similarly, neutralizing antibodies for IL-11 reduced the tumor size. In two Hh-responsive cell lines, ES14 and C3H10T1/2, we found that addition of Smo agonist purmorphamine is sufficient to induce STAT3 phosphorylation at Tyr(705), but this effect was abolished after IL-11Rα down-regulation by shRNAs. Taken together, our results support an important role of the IL-11Rα/STAT3 signaling axis for Hh signaling-mediated signaling and carcinogenesis.
Hedgehog(Hh)通路的激活已知会导致基底细胞癌和髓母细胞瘤的发展,并与许多其他类型的癌症相关,但致癌过程的确切分子机制仍难以捉摸。我们发现,源自表皮表达致癌性 Smo、SmoM2 的皮肤肿瘤具有升高的 IL-11、IL-11Rα 和 STAT3 磷酸化水平(Tyr705)。我们的数据与人类状况的相关性反映在所有检查的人类基底细胞癌都检测到可检测的 STAT3 磷酸化,主要在角质形成细胞中。STAT3 在 Smo 介导的致癌作用中的功能相关性通过表皮特异性敲除 STAT3 揭示。我们表明,从鼠表皮中去除 STAT3 可显著减少 SmoM2 介导的细胞增殖,导致表皮厚度和肿瘤发育显著减少。我们还观察到表皮特异性敲除 STAT3 的小鼠中表皮干细胞/祖细胞群体和细胞周期蛋白 D1 表达显著减少。我们的证据表明,STAT3 信号激活可能由 IL-11/IL-11Rα 信号轴介导。我们表明,在 IL-11Rα 缺失小鼠中诱导 SmoM2 表达后,肿瘤发展减少。同样,针对 IL-11 的中和抗体减少了肿瘤大小。在两个 Hh 反应性细胞系 ES14 和 C3H10T1/2 中,我们发现添加 Smo 激动剂 purmorphamine 足以诱导 STAT3 磷酸化(Tyr705),但在通过 shRNAs 下调 IL-11Rα 后,这种效应被消除。总之,我们的结果支持 IL-11Rα/STAT3 信号轴在 Hh 信号转导介导的信号转导和致癌作用中的重要作用。