Görtz Dieter, Braun Gerald S, Maruta Yuichi, Djudjaj Sonja, van Roeyen Claudia R, Martin Ina V, Küster Andrea, Schmitz-Van de Leur Hildegard, Scheller Jürgen, Ostendorf Tammo, Floege Jürgen, Müller-Newen Gerhard
Institute of Biochemistry and Molecular Biology, RWTH Aachen University, Aachen, Germany.
Division of Nephrology and Immunology, RWTH Aachen University, Aachen, Germany.
Sci Rep. 2015 Oct 1;5:14685. doi: 10.1038/srep14685.
Anti-cytokine therapies have substantially improved the treatment of inflammatory and autoimmune diseases. Cytokine-targeting drugs are usually biologics such as antibodies or other engineered proteins. Production of biologics, however, is complex and intricate and therefore expensive which might limit therapeutic application. To overcome this limitation we developed a strategy that involves the design of an optimized, monogenic cytokine inhibitor and the protein producing capacity of the host. Here, we engineered and characterized a receptor fusion protein, mIL-6-RFP-Fc, for the inhibition of interleukin-6 (IL-6), a well-established target in anti-cytokine therapy. Upon application in mice mIL-6-RFP-Fc inhibited IL-6-induced activation of the transcription factor STAT3 and ERK1/2 kinases in liver and kidney. mIL-6-RFP-Fc is encoded by a single gene and therefore most relevant for gene transfer approaches. Gene transfer through hydrodynamic plasmid delivery in mice resulted in hepatic production and secretion of mIL-6-RFP-Fc into the blood in considerable amounts, blocked hepatic acute phase protein synthesis and improved kidney function in an ischemia and reperfusion injury model. Our study establishes receptor fusion proteins as promising agents in anti-cytokine therapies through gene therapeutic approaches for future targeted and cost-effective treatments. The strategy described here is applicable for many cytokines involved in inflammatory and other diseases.
抗细胞因子疗法已显著改善了炎症性疾病和自身免疫性疾病的治疗。细胞因子靶向药物通常是生物制剂,如抗体或其他工程蛋白。然而,生物制剂的生产复杂且精细,因此成本高昂,这可能会限制其治疗应用。为克服这一限制,我们开发了一种策略,该策略涉及设计一种优化的单基因细胞因子抑制剂以及宿主的蛋白质生产能力。在此,我们构建并表征了一种受体融合蛋白mIL-6-RFP-Fc,用于抑制白细胞介素-6(IL-6),IL-6是抗细胞因子疗法中一个公认的靶点。在小鼠体内应用时,mIL-6-RFP-Fc抑制了IL-6诱导的肝脏和肾脏中转录因子STAT3和ERK1/2激酶的激活。mIL-6-RFP-Fc由单个基因编码,因此与基因转移方法最为相关。通过水动力质粒递送在小鼠体内进行基因转移,导致肝脏产生mIL-6-RFP-Fc并大量分泌到血液中,在缺血再灌注损伤模型中阻断了肝脏急性期蛋白的合成并改善了肾功能。我们的研究通过基因治疗方法,将受体融合蛋白确立为抗细胞因子疗法中未来靶向和经济有效的治疗的有前景的药物。这里描述的策略适用于许多参与炎症和其他疾病的细胞因子。