Unit of Protein Crystallography and Structural Immunology, Navarrabiomed, Pamplona 31008, Spain.
The Lorry I. Lokey Center for Life Sciences and Engineering, Technion - Israel Institute of Technology, Haifa, Israel.
Acta Crystallogr D Struct Biol. 2022 Sep 1;78(Pt 9):1156-1170. doi: 10.1107/S2059798322007677. Epub 2022 Aug 25.
A remarkable number of SARS-CoV-2 variants and other as yet unmonitored lineages harbor amino-acid substitutions with the potential to modulate the interface between the spike receptor-binding domain (RBD) and its receptor ACE2. The naturally occurring Q498Y substitution, which is present in currently circulating SARS-CoV-2 variants, has drawn the attention of several investigations. While computational predictions and in vitro binding studies suggest that Q498Y increases the binding affinity of the spike protein for ACE2, experimental in vivo models of infection have shown that a triple mutant carrying the Q498Y replacement is fatal in mice. To accurately characterize the binding kinetics of the RBD Q498Y-ACE2 interaction, biolayer interferometry analyses were performed. A significant enhancement of the RBD-ACE2 binding affinity relative to a reference SARS-CoV-2 variant of concern carrying three simultaneous replacements was observed. In addition, the RBD Q498Y mutant bound to ACE2 was crystallized. Compared with the structure of its wild-type counterpart, the RBD Q498Y-ACE2 complex reveals the conservation of major hydrogen-bond interactions and a more populated, nonpolar set of contacts mediated by the bulky side chain of Tyr498 that collectively lead to this increase in binding affinity. In summary, these studies contribute to a deeper understanding of the impact of a relevant mutation present in currently circulating SARS-CoV-2 variants which might lead to stronger host-pathogen interactions.
大量的 SARS-CoV-2 变体和其他尚未监测到的谱系都携带有潜在改变刺突受体结合域(RBD)与其受体 ACE2 之间相互作用的氨基酸替换。目前在循环中的 SARS-CoV-2 变体中存在的自然发生的 Q498Y 替换引起了几项研究的关注。虽然计算预测和体外结合研究表明 Q498Y 增加了刺突蛋白与 ACE2 的结合亲和力,但感染的实验体内模型表明,携带 Q498Y 替换的三重突变体在小鼠中是致命的。为了准确描述 RBD Q498Y-ACE2 相互作用的结合动力学,进行了生物层干涉分析。与携带三个同时替换的参考 SARS-CoV-2 变体相比,观察到 RBD-ACE2 结合亲和力的显著增强。此外,RBD Q498Y 突变体与 ACE2 结合并结晶。与野生型相比,RBD Q498Y-ACE2 复合物的结构揭示了主要氢键相互作用的保守性,以及 Tyr498 大侧链介导的更丰富的非极性接触,这些共同导致了结合亲和力的增加。总之,这些研究有助于更深入地了解目前循环中的 SARS-CoV-2 变体中存在的相关突变的影响,这可能导致更强的宿主-病原体相互作用。