Department of Chemistry, University of California, Berkeley, CA 94720, USA.
Proc Natl Acad Sci U S A. 2012 Nov 6;109(45):18378-83. doi: 10.1073/pnas.1208280109. Epub 2012 Oct 24.
Many toxins assemble into oligomers on the surface of cells. Local chemical cues signal and trigger critical rearrangements of the oligomer, inducing the formation of a membrane-fused or channel state. Bacillus anthracis secretes two virulence factors: a tripartite toxin and a poly-γ-d-glutamic acid capsule (γ-DPGA). The toxin's channel-forming component, protective antigen (PA), oligomerizes to create a prechannel that forms toxic complexes upon binding the two other enzyme components, lethal factor (LF) and edema factor (EF). Following endocytosis into host cells, acidic pH signals the prechannel to form the channel state, which translocates LF and EF into the host cytosol. We report γ-DPGA binds to PA, LF, and EF, exhibiting nanomolar avidity for the PA prechannel oligomer. We show PA channel formation requires the pH-dependent disruption of the intra-PA domain-2-domain-4 (D2-D4) interface. γ-DPGA stabilizes the D2-D4 interface, preventing channel formation both in model membranes and cultured mammalian cells. A 1.9-Å resolution X-ray crystal structure of a D2-D4-interface mutant and corresponding functional studies reveal how stability at the intra-PA interface governs channel formation. We also pinpoint the kinetic pH trigger for channel formation to a residue within PA's membrane-insertion loop at the inter-PA D2-D4 interface. Thus, γ-DPGA may function as a chemical cue, signaling that the local environment is appropriate for toxin assembly but inappropriate for channel formation.
许多毒素在细胞表面组装成低聚物。局部化学信号提示并触发低聚物的关键重排,诱导形成膜融合或通道状态。炭疽芽孢杆菌分泌两种毒力因子:三聚体毒素和多聚γ-D-谷氨酸胶囊(γ-DPGA)。毒素的通道形成成分,保护性抗原(PA),寡聚化以创建一个预通道,该通道在结合另外两种酶成分致死因子(LF)和水肿因子(EF)后形成毒性复合物。在进入宿主细胞内吞作用后,酸性 pH 信号提示预通道形成通道状态,将 LF 和 EF 易位到宿主细胞质中。我们报告 γ-DPGA 与 PA、LF 和 EF 结合,对 PA 预通道寡聚体表现出纳摩尔亲和力。我们表明 PA 通道形成需要依赖 pH 的 PA 域 2-域 4(D2-D4)界面内的破坏。γ-DPGA 稳定 D2-D4 界面,防止模型膜和培养的哺乳动物细胞中的通道形成。D2-D4 界面突变体的 1.9 Å分辨率 X 射线晶体结构和相应的功能研究揭示了 PA 界面内的稳定性如何控制通道形成。我们还确定了通道形成的动力学 pH 触发点位于 PA 的跨 PA D2-D4 界面的膜插入环内的一个残基上。因此,γ-DPGA 可能作为化学信号,提示局部环境适合毒素组装但不适合通道形成。