Department of Medicine and.
Department of Biological Sciences, University of California, San Diego, La Jolla, California, USA.
JCI Insight. 2022 Apr 22;7(8):e155761. doi: 10.1172/jci.insight.155761.
Systemic sclerosis (SSc) is a fibrotic autoimmune disease characterized by pathogenic activation of fibroblasts enhanced by local oxidative stress. The tyrosine phosphatase PTP4A1 was identified as a critical promoter of TGF-β signaling in SSc. Oxidative stress is known to functionally inactivate tyrosine phosphatases. Here, we assessed whether oxidation of PTP4A1 modulates its profibrotic action and found that PTP4A1 forms a complex with the kinase SRC in scleroderma fibroblasts, but surprisingly, oxidative stress enhanced rather than reduced PTP4A1's association with SRC and its profibrotic action. Through structural assessment of the oxo-PTP4A1-SRC complex, we unraveled an unexpected mechanism whereby oxidation of a tyrosine phosphatase promotes its function through modification of its protein complex. Considering the importance of oxidative stress in the pathogenesis of SSc and fibrosis, our findings suggest routes for leveraging PTP4A1 oxidation as a potential strategy for developing antifibrotic agents.
系统性硬化症(SSc)是一种纤维化自身免疫性疾病,其特征在于成纤维细胞的病理性激活,这种激活由局部氧化应激增强。酪氨酸磷酸酶 PTP4A1 被鉴定为 SSc 中 TGF-β 信号的关键促进剂。已知氧化应激可使酪氨酸磷酸酶在功能上失活。在这里,我们评估了 PTP4A1 的氧化是否调节其致纤维化作用,并发现 PTP4A1 在硬皮病成纤维细胞中与激酶 SRC 形成复合物,但令人惊讶的是,氧化应激增强而不是降低 PTP4A1 与 SRC 的结合及其致纤维化作用。通过对 oxo-PTP4A1-SRC 复合物的结构评估,我们揭示了一个意想不到的机制,即通过修饰其蛋白质复合物,氧化磷酸酶促进其功能。考虑到氧化应激在 SSc 和纤维化发病机制中的重要性,我们的发现为利用 PTP4A1 氧化作为开发抗纤维化药物的潜在策略提供了途径。