Li Yuening, Gray Elizabeth H, Ross Rosie, Zebochin Irene, Lock Amy, Fedele Laura, Kamajaya Louisa Janice, Marrow Rebecca J, Ryan Sarah, Röderer Pascal, Brüstle Oliver, John Susan, Denk Franziska, Taams Leonie S
Centre for Inflammation Biology & Cancer Immunology, Department of Inflammation Biology, School of Immunology & Microbial Sciences.
Wolfson Sensory, Pain and Regeneration Centre (SPaRC), Guy's Campus, and.
JCI Insight. 2025 May 15;10(12). doi: 10.1172/jci.insight.186646. eCollection 2025 Jun 23.
JAK inhibitors (JAKi) are widely used antiinflammatory drugs. Recent data suggest that JAKi have superior effects on pain reduction in rheumatoid arthritis (RA). However, the underlying mechanisms for this observation are not fully understood. We investigated whether JAKi can act directly on human sensory neurons. We analyzed RNA-seq datasets of sensory neurons and found that they expressed JAK1 and STAT3. Addition of cell-free RA synovial fluid to human induced pluripotent stem cell-derived (iPSC-derived) sensory neurons led to phosphorylation of STAT3 (pSTAT3), which was completely blocked by the JAKi tofacitinib. Compared with paired serum, RA synovial fluid was enriched for the STAT3 signalling cytokines IL-6, IL-11, LIF, IFN-α, and IFN-β, with their requisite receptors present in peripheral nerves postmortem. Accordingly, these recombinant cytokines induced pSTAT3 in iPSC-derived sensory neurons. Furthermore, IL-6 + sIL-6R and LIF upregulated expression of pain-relevant genes with STAT3-binding sites, an effect that was blocked by tofacitinib. LIF also induced neuronal sensitization, highlighting this molecule as a putative pain mediator. Finally, over time, tofacitinib reduced the firing rate of sensory neurons stimulated with RA synovial fluid. Together, these data indicate that JAKi can act directly on human sensory neurons, providing a potential mechanistic explanation for their suggested superior analgesic properties.
JAK抑制剂(JAKi)是广泛使用的抗炎药物。最近的数据表明,JAKi在类风湿性关节炎(RA)的疼痛减轻方面具有卓越效果。然而,这一观察结果的潜在机制尚未完全明确。我们研究了JAKi是否能直接作用于人类感觉神经元。我们分析了感觉神经元的RNA测序数据集,发现它们表达JAK1和STAT3。将无细胞的类风湿性关节炎滑膜液添加到人类诱导多能干细胞衍生(iPSC衍生)的感觉神经元中会导致STAT3磷酸化(pSTAT3),而JAKi托法替布可完全阻断这一过程。与配对血清相比,类风湿性关节炎滑膜液中富含STAT3信号细胞因子IL-6、IL-11、LIF、IFN-α和IFN-β,其必需受体存在于死后的外周神经中。因此,这些重组细胞因子可诱导iPSC衍生的感觉神经元中的pSTAT3。此外,IL-6 + sIL-6R和LIF上调了具有STAT3结合位点的疼痛相关基因的表达,这一效应被托法替布阻断。LIF还诱导了神经元致敏,突出了该分子作为一种假定的疼痛介质的作用。最后,随着时间的推移,托法替布降低了用类风湿性关节炎滑膜液刺激的感觉神经元的放电频率。总之,这些数据表明JAKi可直接作用于人类感觉神经元,为其推测的卓越镇痛特性提供了潜在的机制解释。