Li Weiyun, Xiao Jun, Zhou Xin, Xu Ming, Hu Chaobo, Xu Xiaoyan, Lu Yao, Liu Chang, Xue Shengjie, Nie Lei, Zhang Haibin, Li Zhiqi, Zhang Yanbo, Ji Fu, Hui Lijian, Tao Wufan, Wei Bin, Wang Hongyan
J Clin Invest. 2015 Nov 2;125(11):4239-54. doi: 10.1172/JCI81203. Epub 2015 Oct 12.
Hepatocellular carcinoma (HCC) is frequently associated with pathogen infection-induced chronic inflammation. Large numbers of innate immune cells are present in HCCs and can influence disease outcome. Here, we demonstrated that the tumor suppressor serine/threonine-protein kinase 4 (STK4) differentially regulates TLR3/4/9-mediated inflammatory responses in macrophages and thereby is protective against chronic inflammation-associated HCC. STK4 dampened TLR4/9-induced proinflammatory cytokine secretion but enhanced TLR3/4-triggered IFN-β production via binding to and phosphorylating IL-1 receptor-associated kinase 1 (IRAK1), leading to IRAK1 degradation. Notably, macrophage-specific Stk4 deletion resulted in chronic inflammation, liver fibrosis, and HCC in mice treated with a combination of diethylnitrosamine (DEN) and CCl4, along with either LPS or E. coli infection. STK4 expression was markedly reduced in macrophages isolated from human HCC patients and was inversely associated with the levels of IRAK1, IL-6, and phospho-p65 or phospho-STAT3. Moreover, serum STK4 levels were specifically decreased in HCC patients with high levels of IL-6. In STK4-deficient mice, treatment with an IRAK1/4 inhibitor after DEN administration reduced serum IL-6 levels and liver tumor numbers to levels similar to those observed in the control mice. Together, our results suggest that STK4 has potential as a diagnostic biomarker and therapeutic target for inflammation-induced HCC.
肝细胞癌(HCC)常与病原体感染诱导的慢性炎症相关。HCC中存在大量先天性免疫细胞,它们可影响疾病结局。在此,我们证明肿瘤抑制因子丝氨酸/苏氨酸蛋白激酶4(STK4)可差异性调节巨噬细胞中TLR3/4/9介导的炎症反应,从而对慢性炎症相关的HCC具有保护作用。STK4可抑制TLR4/9诱导的促炎细胞因子分泌,但通过与白细胞介素-1受体相关激酶1(IRAK1)结合并使其磷酸化,增强TLR3/4触发的IFN-β产生,导致IRAK1降解。值得注意的是,在接受二乙基亚硝胺(DEN)和四氯化碳(CCl4)联合处理以及LPS或大肠杆菌感染的小鼠中,巨噬细胞特异性Stk4缺失导致慢性炎症、肝纤维化和HCC。从人类HCC患者分离的巨噬细胞中STK4表达明显降低,且与IRAK1、IL-6以及磷酸化p65或磷酸化STAT3的水平呈负相关。此外,IL-6水平高的HCC患者血清STK4水平特异性降低。在STK4缺陷小鼠中,DEN给药后用IRAK1/4抑制剂治疗可使血清IL-6水平和肝肿瘤数量降至与对照小鼠相似的水平。总之,我们的结果表明STK4有潜力作为炎症诱导的HCC的诊断生物标志物和治疗靶点。