Riedlinger Tabea, Haas Jana, Busch Julia, van de Sluis Bart, Kracht Michael, Schmitz M Lienhard
Institute of Biochemistry, Justus-Liebig-University, D-35392 Giessen, Germany.
Department of Pediatrics, Molecular Genetics Section, University of Groningen, University Medical Center Groningen, Antonius Deusinglaan 1, 9713 AV, Groningen, The Netherlands.
Biomedicines. 2018 Mar 19;6(1):36. doi: 10.3390/biomedicines6010036.
NF-κB signaling pathways play an important role in the regulation of cellular immune and stress responses. Aberrant NF-κB activity has been implicated in almost all the steps of cancer development and many of the direct and indirect contributions of this transcription factor system for oncogenesis were revealed in the recent years. The indirect contributions affect almost all hallmarks and enabling characteristics of cancer, but NF-κB can either promote or antagonize these tumor-supportive functions, thus prohibiting global NF-κB inhibition. The direct effects are due to mutations of members of the NF-κB system itself. These mutations typically occur in upstream components that lead to the activation of NF-κB together with further oncogenesis-promoting signaling pathways. In contrast, mutations of the downstream components, such as the DNA-binding subunits, contribute to oncogenic transformation by affecting NF-κB-driven transcriptional output programs. Here, we discuss the features of recently identified oncogenic RelA fusion proteins and the characterization of pathways that are regulating the transcriptional activity of NF-κB by regulatory phosphorylations. As NF-κB's central role in human physiology prohibits its global inhibition, these auxiliary or cell type-specific NF-κB regulating pathways are potential therapeutic targets.
核因子-κB(NF-κB)信号通路在细胞免疫和应激反应的调节中发挥着重要作用。近年来,NF-κB异常激活几乎与癌症发展的所有步骤都有关联,并且该转录因子系统对肿瘤发生的许多直接和间接作用也已被揭示。间接作用几乎影响癌症的所有特征和促成特性,但NF-κB既可以促进也可以拮抗这些肿瘤支持性功能,因此禁止对NF-κB进行全面抑制。直接作用是由于NF-κB系统成员自身发生突变。这些突变通常发生在上游成分中,导致NF-κB激活并伴随进一步促进肿瘤发生的信号通路。相反,下游成分(如DNA结合亚基)的突变通过影响NF-κB驱动的转录输出程序而导致致癌转化。在此,我们讨论最近鉴定出的致癌性RelA融合蛋白的特征以及通过调节性磷酸化来调节NF-κB转录活性的信号通路的特征。由于NF-κB在人类生理学中的核心作用禁止对其进行全面抑制,这些辅助性或细胞类型特异性的NF-κB调节通路是潜在的治疗靶点。