Department of Internal Medicine, School of Medicine, Kangwon National University, Chuncheon 24341, Korea.
Graduate School of Biomedical Science and Engineering, Hanyang University, Seoul 04763, Korea.
Int J Mol Sci. 2020 Oct 29;21(21):8090. doi: 10.3390/ijms21218090.
Ubiquitination and deubiquitination play a fundamental role in the signaling pathways associated with innate and adaptive immune responses. Macrophages are key sentinels for the host defense, triggering antiviral and inflammatory responses against various invading pathogens. Macrophages recognize the genetic material of these pathogens as pathogen-associated molecular patterns (PAMPs) and danger-associated molecular patterns (DAMPs) through the activation of its pattern recognition receptors (PRRs), initiating the cascade of immune signaling, which leads to the production of pro- and anti-inflammatory cytokines that initiates the appropriate immune response. Macrophage-mediated immune response is highly regulated and tightly controlled by the ubiquitin system since its abnormal activation or dysregulation may result in the severe pathogenesis of numerous inflammatory and autoimmune diseases. Deubiquitinating enzymes (DUBs) play a crucial role in reversing the ubiquitination and controlling the magnitude of the immune response. During infection, pathogens manipulate the host defense system by regulating DUBs to obtain nutrients and increase proliferation. Indeed, the regulation of DUBs by small molecule inhibitors has been proposed as an excellent way to control aberrant activation of immune signaling molecules. This review is focused on the complex role of DUBs in macrophage-mediated immune response, exploring the potential use of DUBs as therapeutic targets in autoimmune and inflammatory diseases by virtue of small molecule DUB inhibitors.
泛素化和去泛素化在先天和适应性免疫反应相关的信号通路中起着至关重要的作用。巨噬细胞是宿主防御的关键哨兵,针对各种入侵病原体触发抗病毒和炎症反应。巨噬细胞通过其模式识别受体(PRRs)识别这些病原体的遗传物质,即病原体相关分子模式(PAMPs)和危险相关分子模式(DAMPs),启动免疫信号级联反应,导致产生促炎和抗炎细胞因子,从而引发适当的免疫反应。由于其异常激活或失调可能导致许多炎症和自身免疫性疾病的严重发病机制,因此泛素系统对巨噬细胞介导的免疫反应具有高度调节和严格控制作用。去泛素化酶(DUBs)在逆转泛素化和控制免疫反应幅度方面起着至关重要的作用。在感染过程中,病原体通过调节 DUBs 来获取营养和增加增殖,从而操纵宿主防御系统。事实上,小分子抑制剂对 DUBs 的调控已被提出作为控制免疫信号分子异常激活的一种极好方法。本综述重点探讨了 DUBs 在巨噬细胞介导的免疫反应中的复杂作用,通过小分子 DUB 抑制剂探索将 DUBs 作为自身免疫和炎症性疾病治疗靶点的潜力。