Arthritis and Tissue Degeneration Program, Autoimmunity and Inflammation Program, Hospital for Special Surgery, Weill Cornell University, New York, New York, USA.
J Clin Invest. 2013 Feb;123(2):928-32. doi: 10.1172/JCI66168. Epub 2013 Jan 25.
iRHOM2, encoded by the gene Rhbdf2, regulates the maturation of the TNF-α convertase (TACE), which controls shedding of TNF-α and its biological activity in vivo. TACE is a potential target to treat TNF-α-dependent diseases, such as rheumatoid arthritis, but there are concerns about potential side effects, because TACE also protects the skin and intestinal barrier by activating EGFR signaling. Here we report that inactivation of Rhbdf2 allows tissue-specific regulation of TACE by selectively preventing its maturation in immune cells, without affecting its homeostatic functions in other tissues. The related iRHOM1, which is widely expressed, except in hematopoietic cells, supported TACE maturation and shedding of the EGFR ligand TGF-α in Rhbdf2-deficient cells. Remarkably, mice lacking Rhbdf2 were protected from K/BxN inflammatory arthritis to the same extent as mice lacking TACE in myeloid cells or Tnfa-deficient mice. In probing the underlying mechanism, we found that two main drivers of K/BxN arthritis, complement C5a and immune complexes, stimulated iRHOM2/TACE-dependent shedding of TNF-α in mouse and human cells. These data demonstrate that iRHOM2 and myeloid-expressed TACE play a critical role in inflammatory arthritis and indicate that iRHOM2 is a potential therapeutic target for selective inactivation of TACE in myeloid cells.
iRHOM2,由基因 Rhbdf2 编码,调节 TNF-α 转化酶(TACE)的成熟,后者控制 TNF-α 的脱落及其在体内的生物学活性。TACE 是治疗 TNF-α 依赖性疾病(如类风湿关节炎)的潜在靶点,但人们担心可能会产生副作用,因为 TACE 通过激活 EGFR 信号通路还能保护皮肤和肠道屏障。我们报告称,Rhbdf2 的失活允许 TACE 在组织特异性水平受到调控,其方法是选择性地阻止其在免疫细胞中的成熟,而不影响其在其他组织中的稳态功能。广泛表达但不包括造血细胞中的相关 iRHOM1 支持 Rhbdf2 缺陷细胞中 TACE 的成熟和 EGFR 配体 TGF-α的脱落。值得注意的是,缺乏 Rhbdf2 的小鼠在 K/BxN 炎症性关节炎中的保护程度与髓样细胞中缺乏 TACE 或 Tnfa 缺陷的小鼠相同。在探究潜在机制时,我们发现 K/BxN 关节炎的两个主要驱动因素,补体 C5a 和免疫复合物,刺激了小鼠和人细胞中 iRHOM2/TACE 依赖性 TNF-α的脱落。这些数据表明 iRHOM2 和髓样细胞表达的 TACE 在炎症性关节炎中起着关键作用,并表明 iRHOM2 是选择性失活髓样细胞中 TACE 的潜在治疗靶点。