Department of Molecular Immunology, Institute of Industrial Science, The University of Tokyo, 153-8505 Tokyo, Japan.
Department of Inflammology, Research Center for Advanced Science and Technology, The University of Tokyo, 153-0041 Tokyo, Japan.
Proc Natl Acad Sci U S A. 2019 Nov 19;116(47):23653-23661. doi: 10.1073/pnas.1915326116. Epub 2019 Nov 6.
The activation of innate immune receptors by pathogen-associated molecular patterns (PAMPs) is central to host defense against infections. On the other hand, these receptors are also activated by immunogenic damage-associated molecular patterns (DAMPs), typically released from dying cells, and the activation can evoke chronic inflammatory or autoimmune disorders. One of the best known receptors involved in the immune pathogenesis is Toll-like receptor 7 (TLR7), which recognizes RNA with single-stranded structure. However, the causative DAMP RNA(s) in the pathogenesis has yet to be identified. Here, we first developed a chemical compound, termed KN69, that suppresses autoimmunity in several established mouse models. A subsequent search for KN69-binding partners led to the identification of U11 small nuclear RNA (U11snRNA) as a candidate DAMP RNA involved in TLR7-induced autoimmunity. We then showed that U11snRNA robustly activated the TLR7 pathway in vitro and induced arthritis disease in vivo. We also found a correlation between high serum level of U11snRNA and autoimmune diseases in human subjects and established mouse models. Finally, by revealing the structural basis for U11snRNA's ability to activate TLR7, we developed more potent TLR7 agonists and TLR7 antagonists, which may offer new therapeutic approaches for autoimmunity or other immune-driven diseases. Thus, our study has revealed a hitherto unknown immune function of U11snRNA, providing insight into TLR7-mediated autoimmunity and its potential for further therapeutic applications.
先天免疫受体被病原体相关分子模式(PAMPs)激活是宿主抵御感染的核心。另一方面,这些受体也被免疫原性损伤相关分子模式(DAMPs)激活,这些 DAMPs 通常从死亡细胞中释放出来,其激活会引发慢性炎症或自身免疫性疾病。涉及免疫发病机制的最著名受体之一是 Toll 样受体 7(TLR7),它识别具有单链结构的 RNA。然而,发病机制中导致 DAMPs 产生的 RNA 尚未被确定。在这里,我们首先开发了一种化学化合物,称为 KN69,它可以抑制几种已建立的小鼠模型中的自身免疫。随后寻找 KN69 的结合伙伴导致 U11 小核 RNA(U11snRNA)被鉴定为参与 TLR7 诱导自身免疫的候选 DAMPs RNA。然后我们表明 U11snRNA 在体外强烈激活 TLR7 途径,并在体内诱导关节炎疾病。我们还发现人类受试者和建立的小鼠模型中血清 U11snRNA 水平与自身免疫性疾病之间存在相关性。最后,通过揭示 U11snRNA 激活 TLR7 的结构基础,我们开发了更有效的 TLR7 激动剂和 TLR7 拮抗剂,这可能为自身免疫或其他免疫驱动的疾病提供新的治疗方法。因此,我们的研究揭示了 U11snRNA 迄今未知的免疫功能,为 TLR7 介导的自身免疫及其进一步治疗应用提供了新的见解。