Montana Biotechnology Center, Science Complex Room 221, The University of Montana, Missoula, MT 59812, USA.
J Virol. 2010 Jun;84(12):6119-29. doi: 10.1128/JVI.02700-09. Epub 2010 Apr 14.
The arenavirus envelope glycoprotein (GPC) initiates infection in the host cell through pH-induced fusion of the viral and endosomal membranes. As in other class I viral fusion proteins, this process proceeds through a structural reorganization in GPC in which the ectodomain of the transmembrane fusion subunit (G2) engages the host cell membrane and subsequently refolds to form a highly stable six-helix bundle structure that brings the two membranes into apposition for fusion. Here, we describe a G2-directed monoclonal antibody, F100G5, that prevents membrane fusion by binding to an intermediate form of the protein on the fusion pathway. Inhibition of syncytium formation requires that F100G5 be present concomitant with exposure of GPC to acidic pH. We show that F100G5 recognizes neither the six-helix bundle nor the larger trimer-of-hairpins structure in the postfusion form of G2. Rather, Western blot analysis using recombinant proteins and a panel of alanine-scanning GPC mutants revealed that F100G5 binding is dependent on an invariant lysine residue (K283) near the N terminus of G2, in the so-called fusion peptide that inserts into the host cell membrane during the fusion process. The F100G5 epitope is located in the internal segment of the bipartite GPC fusion peptide, which also contains four conserved cysteine residues, raising the possibility that this fusion peptide may be highly structured. Collectively, our studies indicate that F100G5 identifies an on-path intermediate form of GPC. Binding to the transiently exposed fusion peptide may interfere with G2 insertion into the host cell membrane. Strategies to effectively target fusion peptide function in the endosome may lead to novel classes of antiviral agents.
沙粒病毒包膜糖蛋白(GPC)通过病毒和内体膜的 pH 诱导融合在宿主细胞中引发感染。与其他 I 类病毒融合蛋白一样,该过程通过 GPC 的结构重排进行,其中跨膜融合亚基(G2)的外域与宿主细胞膜结合,随后重新折叠形成高度稳定的六螺旋束结构,使两个膜并置融合。在这里,我们描述了一种针对 G2 的单克隆抗体 F100G5,它通过结合融合途径中的中间形式的蛋白质来阻止膜融合。抑制合胞体形成需要 F100G5 与 GPC 暴露于酸性 pH 同时存在。我们表明,F100G5 既不识别六螺旋束,也不识别 G2 融合后形式中的较大三螺旋发夹结构。相反,使用重组蛋白和一组丙氨酸扫描 GPC 突变体的 Western blot 分析表明,F100G5 的结合依赖于 G2 近 N 端的一个不变的赖氨酸残基(K283),在融合过程中,该赖氨酸残基插入宿主细胞膜的融合肽中。F100G5 表位位于二部分 GPC 融合肽的内部片段中,该片段还包含四个保守的半胱氨酸残基,这表明该融合肽可能具有高度的结构。总的来说,我们的研究表明,F100G5 鉴定了 GPC 的一个中间形式。与短暂暴露的融合肽结合可能会干扰 G2 插入宿主细胞膜。有效靶向内体中融合肽功能的策略可能会导致新型抗病毒药物的出现。