Foka Pelagia, Dimitriadis Alexios, Kyratzopoulou Eleni, Giannimaras Dionysios A, Sarno Stefania, Simos George, Georgopoulou Urania, Mamalaki Avgi
Laboratory of Molecular Biology and Immunobiotechnology, Department of Biochemistry, Hellenic Pasteur Institute, Athens, Greece.
Cell Mol Life Sci. 2014 Nov;71(21):4243-58. doi: 10.1007/s00018-014-1621-4. Epub 2014 Apr 10.
Hepatitis C virus (HCV) infection is associated with hepatic iron overload and elevated serum iron that correlate to poor antiviral responses. Hepcidin (HAMP), a 25-aa cysteine-rich liver-specific peptide, controls iron homeostasis. Its expression is up-regulated in inflammation and iron excess. HCV-mediated hepcidin regulation remains controversial. Chronic HCV patients possess relatively low hepcidin levels; however, elevated HAMP mRNA has been reported in HCV core transgenic mice and HCV replicon-expressing cells. We investigated the effect of HCV core protein on HAMP gene expression and delineated the complex interplay of molecular mechanisms involved. HCV core protein up-regulated HAMP promoter activity, mRNA, and secreted protein levels. Enhanced promoter activity was abolished by co-transfections of core with HAMP promoter constructs containing mutated/deleted BMP and STAT binding sites. Dominant negative constructs, pharmacological inhibitors, and silencing experiments against STAT3 and SMAD4 confirmed the participation of both pathways in HAMP gene regulation by core protein. STAT3 and SMAD4 expression levels were found increased in the presence of HCV core, which orchestrated SMAD4 translocation into the nucleus and STAT3 phosphorylation. To further understand the mechanisms governing the core effect, the role of the JAK/STAT-activating kinase CK2 was investigated. A CK2-dominant negative construct, a CK2-specific inhibitor, and RNAi interference abrogated the core-induced increase on HAMP promoter activity, mRNA, and protein levels, while CK2 acted in synergy with core to significantly enhance HAMP gene expression. Therefore, HCV core up-regulates HAMP gene transcription via a complex signaling network that requires both SMAD/BMP and STAT3 pathways and CK2 involvement.
丙型肝炎病毒(HCV)感染与肝脏铁过载及血清铁升高有关,而这与抗病毒反应不佳相关。铁调素(HAMP)是一种富含25个氨基酸的肝脏特异性半胱氨酸肽,可控制铁稳态。其表达在炎症和铁过量时会上调。HCV介导的铁调素调节仍存在争议。慢性HCV患者的铁调素水平相对较低;然而,在HCV核心转基因小鼠和表达HCV复制子的细胞中已报道铁调素mRNA升高。我们研究了HCV核心蛋白对HAMP基因表达的影响,并阐述了所涉及分子机制的复杂相互作用。HCV核心蛋白上调了HAMP启动子活性、mRNA和分泌蛋白水平。通过将核心与含有突变/缺失的骨形态发生蛋白(BMP)和信号转导及转录激活因子(STAT)结合位点的HAMP启动子构建体共转染,增强的启动子活性被消除。针对STAT3和SMAD4的显性负性构建体、药理抑制剂和沉默实验证实了这两条途径均参与核心蛋白对HAMP基因的调节。在存在HCV核心的情况下,发现STAT3和SMAD4的表达水平增加,这促使SMAD4易位至细胞核并使STAT3磷酸化。为了进一步了解控制核心效应的机制,研究了JAK/STAT激活激酶CK2的作用。一个CK2显性负性构建体、一种CK2特异性抑制剂和RNA干扰消除了核心诱导的HAMP启动子活性、mRNA和蛋白水平的增加,而CK2与核心协同作用可显著增强HAMP基因表达。因此,HCV核心通过一个复杂的信号网络上调HAMP基因转录,该网络需要SMAD/BMP和STAT3途径以及CK2的参与。