School of Biological Sciences, University of Utah, Salt Lake City, Utah, USA.
Protein Sci. 2024 Dec;33(12):e5209. doi: 10.1002/pro.5209.
The experimental challenges posed by integral membrane proteins hinder molecular understanding of transmembrane signaling mechanisms. Here, we exploited protein crosslinking assays in living cells to follow conformational and dynamic stimulus signals in Tsr, the Escherichia coli serine chemoreceptor. Tsr mediates serine chemotaxis by integrating transmembrane serine-binding inputs with adaptational modifications of a methylation helix bundle to regulate a signaling kinase at the cytoplasmic tip of the receptor molecule. We created cysteine replacements at Tsr residues adjacent to hydrophobic packing faces of the bundle helices and crosslinked them with a cell-permeable, bifunctional thiol-reagent. We identified an extensively crosslinked dynamic junction midway through the methylation helix bundle that seemed uniquely poised to respond to serine signals. We explored its role in mediating signaling shifts between different packing arrangements of the bundle helices by measuring crosslinking in receptor molecules with apposed pairs of cysteine reporters in each subunit and assessing their signaling behaviors with an in vivo kinase assay. In the absence of serine, the bundle helices evinced compact kinase-ON packing arrangements; in the presence of serine, the dynamic junction destabilized adjacent bundle segments and shifted the bundle to an expanded, less stable kinase-OFF helix-packing arrangement. AlphaFold models of kinase-active Tsr showed a prominent bulge and kink at the dynamic junction that might antagonize stable structure at the receptor tip. Serine stimuli might inhibit kinase activity by shifting the bundle to a less stably-packed conformation that relaxes structural strain at the receptor tip, thereby allowing it to stabilize and freeze kinase activity.
整联膜蛋白所带来的实验挑战阻碍了对跨膜信号转导机制的分子理解。在这里,我们利用活细胞中的蛋白交联实验,跟踪 Tsr(大肠杆菌丝氨酸化学感受器)中的构象和动态刺激信号。Tsr 通过整合跨膜丝氨酸结合输入与甲基化螺旋束的适应性修饰,来调节受体分子细胞质尖端的信号激酶,从而介导丝氨酸化学趋化作用。我们在 Tsr 残基处创建了临近于螺旋束疏水面的半胱氨酸替换,并将它们与一种细胞通透的双功能巯基试剂交联。我们鉴定出一个广泛交联的动态连接点,位于甲基化螺旋束的中间,似乎特别适合响应丝氨酸信号。我们通过测量每个亚基中相邻的半胱氨酸报告器对的受体分子中的交联,并使用体内激酶测定法评估它们的信号行为,来探索其在介导螺旋束不同包装排列之间的信号转导变化中的作用。在没有丝氨酸的情况下,螺旋束表现出紧凑的激酶开启包装排列;在有丝氨酸的情况下,动态连接点使相邻的螺旋束段不稳定,并将螺旋束转移到扩展的、不太稳定的激酶关闭螺旋包装排列。激酶活性的 Tsr 的 AlphaFold 模型显示出在动态连接点处有一个突出的凸起和拐点,这可能会拮抗受体尖端的稳定结构。丝氨酸刺激可能通过将螺旋束转移到不太稳定的包装构象来抑制激酶活性,从而缓解受体尖端的结构应变,使其能够稳定并冻结激酶活性。