Zalevsky Jonathan, Secher Thomas, Ezhevsky Sergei A, Janot Laure, Steed Paul M, O'Brien Christopher, Eivazi Araz, Kung James, Nguyen Duc-Hanh T, Doberstein Stephen K, Erard François, Ryffel Bernhard, Szymkowski David E
Xencor, Monrovia, CA 91016, USA.
J Immunol. 2007 Aug 1;179(3):1872-83. doi: 10.4049/jimmunol.179.3.1872.
TNF is a pleiotropic cytokine required for normal development and function of the immune system; however, TNF overexpression also induces inflammation and is associated with autoimmune diseases. TNF exists as both a soluble and a transmembrane protein. Genetic studies in mice have suggested that inflammation in disease models involves soluble TNF (solTNF) and that maintenance of innate immune function involves transmembrane TNF (tmTNF). These findings imply that selective pharmacologic inhibition of solTNF may be anti-inflammatory and yet preserve innate immunity to infection. To address this hypothesis, we now describe dominant-negative inhibitors of TNF (DN-TNFs) as a new class of biologics that selectively inhibits solTNF. DN-TNFs blocked solTNF activity in human and mouse cells, a human blood cytokine release assay, and two mouse arthritis models. In contrast, DN-TNFs neither inhibited the activity of human or mouse tmTNF nor suppressed innate immunity to Listeria infection in mice. These results establish DN-TNFs as the first selective inhibitors of solTNF, demonstrate that inflammation in mouse arthritis models is primarily driven by solTNF, and suggest that the maintenance of tmTNF activity may improve the therapeutic index of future anti-inflammatory agents.
肿瘤坏死因子(TNF)是免疫系统正常发育和功能所必需的多效性细胞因子;然而,TNF的过度表达也会引发炎症,并与自身免疫性疾病相关。TNF以可溶性蛋白和跨膜蛋白两种形式存在。对小鼠的基因研究表明,疾病模型中的炎症涉及可溶性TNF(solTNF),而固有免疫功能的维持涉及跨膜TNF(tmTNF)。这些发现意味着,对solTNF进行选择性药理抑制可能具有抗炎作用,同时保留对感染的固有免疫力。为了验证这一假设,我们现在描述了一种新型生物制剂——TNF显性负性抑制剂(DN-TNFs),它能选择性抑制solTNF。DN-TNFs在人和小鼠细胞、人血细胞因子释放试验以及两种小鼠关节炎模型中均能阻断solTNF的活性。相比之下,DN-TNFs既不抑制人或小鼠tmTNF的活性,也不抑制小鼠对李斯特菌感染的固有免疫力。这些结果确立了DN-TNFs作为首个solTNF选择性抑制剂的地位,证明小鼠关节炎模型中的炎症主要由solTNF驱动,并表明维持tmTNF活性可能会提高未来抗炎药物的治疗指数。