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SHP2变构抑制剂SHP099通过调节IL-17RA信号通路减轻类干燥综合征动物的炎症并恢复唾液腺功能。

SHP2 Allosteric Inhibitor SHP099 Alleviates Inflammation and Restores Salivary Gland Function in Sjögren's Disease-like Animals via Regulation of the IL-17RA Signaling Pathway.

作者信息

Wang Simin, Weng Xiuhong, Liu Chang, Cheng Bo

机构信息

Department of Stomatology, Zhongnan Hospital of Wuhan University, China.

Department of Stomatology, Zhongnan Hospital of Wuhan University, China.

出版信息

Int Immunopharmacol. 2025 Aug 28;161:114986. doi: 10.1016/j.intimp.2025.114986. Epub 2025 Jun 3.

Abstract

Salivary gland (SG) dysfunction is a hallmark manifestation of Sjögren's disease (SjD). While SHP2 has been implicated in several autoimmune diseases, its specific function in SjD remains to be elucidated. Here, we investigated the involvement of SHP2 in SjD-induced SG damage and elucidate the underlying molecular mechanisms. Our findings revealed that SHP2 is elevated in SG tissues of SjD patients and SjD-like animals, with predominant localization to salivary gland epithelial cells (SGECs) of acini and ducts. Notably, pharmacological inhibition of SHP2 with the allosteric inhibitor SHP099 significantly alleviates SG histopathological damage and reduces inflammatory cell infiltration in SjD-like animals. In vitro studies in the human SGEC line A253 revealed that SHP2 inhibition attenuated poly(I:C)-induced SGEC apoptosis and proinflammatory cytokine production. Mechanistically, SHP099 treatment disrupted the IL-17RA/ACT1/TRAF6 signaling axis, phenocopying the effects of SHP2 knockdown and direct IL-17R antagonism, which leads to downregulation of JAK/STAT3 and NF-κB pathways. Collectively, our findings highlight the significant involvement of SHP2 in the pathogenesis of SjD and suggest that targeting SHP2 or its downstream signaling pathways may represent a promising therapeutic approach for SjD treatment.

摘要

唾液腺(SG)功能障碍是干燥综合征(SjD)的标志性表现。虽然SHP2已被证明与多种自身免疫性疾病有关,但其在SjD中的具体功能仍有待阐明。在此,我们研究了SHP2在SjD诱导的唾液腺损伤中的作用,并阐明其潜在的分子机制。我们的研究结果显示,SHP2在SjD患者和类SjD动物的唾液腺组织中升高,主要定位于腺泡和导管的唾液腺上皮细胞(SGECs)。值得注意的是,用变构抑制剂SHP099对SHP2进行药理抑制可显著减轻类SjD动物的唾液腺组织病理学损伤,并减少炎症细胞浸润。在人唾液腺上皮细胞系A253中的体外研究表明,抑制SHP2可减弱聚肌苷酸-聚胞苷酸(poly(I:C))诱导的唾液腺上皮细胞凋亡和促炎细胞因子的产生。机制上,SHP099处理破坏了IL-17RA/ACT1/TRAF6信号轴,模拟了SHP2敲低和直接IL-17R拮抗的效果,从而导致JAK/STAT3和NF-κB信号通路的下调。总的来说,我们的数据突出了SHP2在SjD发病机制中的重要作用,并表明靶向SHP2或其下游信号通路可能是一种有前景的SjD治疗方法。

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