Pitsillou Eleni, El-Osta Assam, Hung Andrew, Karagiannis Tom C
Epigenomic Medicine Laboratory at prospED Polytechnic, Carlton, VIC 3053, Australia.
School of Science, STEM College, RMIT University, Melbourne, VIC 3001, Australia.
Biomolecules. 2025 Feb 18;15(2):301. doi: 10.3390/biom15020301.
The emergence of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) variants poses an ongoing threat to the efficacy of vaccines and therapeutic antibodies. Mutations predominantly affect the receptor-binding domain (RBD) of the spike protein, which mediates viral entry. The RBD is also a major target of monoclonal antibodies that were authorised for use during the pandemic. In this study, an in silico approach was used to investigate the mutational landscape of SARS-CoV-2 RBD variants, including currently circulating Omicron subvariants. A total of 40 single-point mutations were assessed for their potential effect on protein stability and dynamics. Destabilising effects were predicted for mutations such as L455S and F456L, while stabilising effects were predicted for mutations such as R346T. Conformational B-cell epitope predictions were subsequently performed for wild-type (WT) and variant RBDs. Mutations from SARS-CoV-2 variants were located within the predicted epitope residues and the epitope regions were found to correspond to the sites targeted by therapeutic antibodies. Furthermore, homology models of the RBD of SARS-CoV-2 variants were generated and were utilised for protein-antibody docking. The binding characteristics of 10 monoclonal antibodies against WT and 14 SARS-CoV-2 variants were evaluated. Through evaluating the binding affinities, interactions, and energy contributions of RBD residues, mutations that were contributing to viral evasion were identified. The findings from this study provide insight into the structural and molecular mechanisms underlying neutralising antibody evasion. Future antibody development could focus on broadly neutralising antibodies, engineering antibodies with enhanced binding affinity, and targeting spike protein regions beyond the RBD.
严重急性呼吸综合征冠状病毒2(SARS-CoV-2)变体的出现对疫苗和治疗性抗体的疗效构成了持续威胁。突变主要影响刺突蛋白的受体结合域(RBD),该结构域介导病毒进入。RBD也是大流行期间获批使用的单克隆抗体的主要靶点。在本研究中,采用计算机模拟方法研究了SARS-CoV-2 RBD变体的突变情况,包括目前正在传播的奥密克戎亚变体。共评估了40个单点突变对蛋白质稳定性和动力学的潜在影响。预测L455S和F456L等突变具有去稳定作用,而R346T等突变具有稳定作用。随后对野生型(WT)和变体RBD进行了构象性B细胞表位预测。SARS-CoV-2变体的突变位于预测的表位残基内,且发现表位区域与治疗性抗体靶向的位点相对应。此外,还生成了SARS-CoV-2变体RBD的同源模型,并将其用于蛋白质-抗体对接。评估了10种针对WT和14种SARS-CoV-2变体的单克隆抗体的结合特性。通过评估RBD残基的结合亲和力、相互作用和能量贡献,确定了导致病毒逃逸的突变。本研究结果为中和抗体逃逸的结构和分子机制提供了见解。未来的抗体开发可侧重于广泛中和抗体、工程化具有增强结合亲和力的抗体以及靶向RBD以外的刺突蛋白区域。