Department of Biomedical Sciences, Korea University College of Medicine, Seoul, 02841, Korea.
Neurotherapeutics. 2023 Jan;20(1):325-337. doi: 10.1007/s13311-022-01327-3. Epub 2022 Nov 9.
The function of peripheral nociceptors is frequently tuned by the action of G protein-coupled receptors (GPRs) that are expressed in them, which contribute to pain alteration. Expanding new information on such GPRs and predicting their potential outcomes can help to construct new analgesic strategies based on their modulations. In this context, we attempted to present a new GPR not yet acknowledged for its pain association. Gpr83 exhibits relatively high expressions in the peripheral nervous system compared to other tissues when we mined and reconstructed Gene Expression Omnibus (GEO) metadata, which we confirmed using immunohistochemistry on murine dorsal root ganglia (DRG). When Gpr83 expression was silenced in DRG, neuronal and behavioral nociception were all downregulated. Pathologic pain in hind paw inflammation and chemotherapy-induced peripheral neuropathy were also alleviated by this Gpr83 knockdown. Dependent on exposure time, the application of a known endogenous Gpr83 ligand PEN showed differential effects on nociceptor responses in vitro. Localized PEN administration mitigated pain in vivo, probably following Gq/11-involved GPR downregulation caused by the relatively constant exposure. Collectively, this study suggests that Gpr83 action contributes to the tuning of peripheral pain sensitivity and thus indicates that Gpr83 can be among the potential GPR targets for pain modulation.
外周伤害感受器的功能经常受到其表达的 G 蛋白偶联受体 (GPR) 的调节,这些受体有助于疼痛的改变。扩展关于这些 GPR 的新信息,并预测它们的潜在结果,可以帮助基于它们的调节构建新的镇痛策略。在这种情况下,我们试图介绍一种尚未被认为与其疼痛有关的新 GPR。当我们挖掘和重建基因表达综合数据库 (GEO) 元数据时,Gpr83 在周围神经系统中的表达相对高于其他组织,我们在小鼠背根神经节 (DRG) 上的免疫组织化学中证实了这一点。当 DRG 中的 Gpr83 表达被沉默时,神经元和行为性疼痛均被下调。这种 Gpr83 敲低也减轻了后爪炎症和化疗诱导的周围神经病变中的病理性疼痛。根据暴露时间的不同,已知内源性 Gpr83 配体 PEN 的应用对体外伤害感受器反应表现出不同的影响。局部 PEN 给药减轻了体内疼痛,可能是由于相对恒定的暴露导致 Gq/11 参与的 GPR 下调所致。总的来说,这项研究表明 Gpr83 作用有助于外周疼痛敏感性的调节,因此表明 Gpr83 可以成为潜在的疼痛调节 GPR 靶点之一。