Department of Pharmaceutical Sciences, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of Colorado Anschutz Medical Campus, Aurora, CO, USA.
Department of Pharmaceutical Sciences, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of Colorado Anschutz Medical Campus, Aurora, CO, USA.
J Mol Biol. 2022 Jul 15;434(13):167622. doi: 10.1016/j.jmb.2022.167622. Epub 2022 May 6.
Among the five known SARS-CoV-2 variants of concern, Delta is the most virulent leading to severe symptoms and increased mortality among infected people. Our study seeks to examine how the biophysical parameters of the Delta variant correlate to the clinical observations. Receptor binding domain (RBD) is the first point of contact with the human host cells and is the immunodominant form of the spike protein. Delta variant RBD contains two novel mutations L452R and T478K. We examined the effect of single as well as the double mutations on RBD expression in human Expi293 cells, RBD stability using urea and thermal denaturation, and RBD binding to angiotensin converting enzyme 2 (ACE2) receptor and to neutralizing antibodies using isothermal titration calorimetry. Delta variant RBD showed significantly higher expression compared to the wild-type RBD, and the increased expression is due to L452R mutation. Despite their non-conservative nature, none of the mutations significantly affected RBD structure and stability. All mutants showed similar binding affinity to ACE2 and to Class 1 antibodies (CC12.1 and LY-CoV016) as that of the wild-type. Delta double mutant L452R/T478K showed no binding to Class 2 antibodies (P2B-2F6 and LY-CoV555) and a hundred-fold weaker binding to a Class 3 antibody (REGN10987), and the decreased antibody binding is determined by the L452R mutation. These results indicate that the immune escape from neutralizing antibodies, rather than increased receptor binding, is the main biophysical parameter that determined the fitness landscape of the Delta variant RBD.
在五种已知的 SARS-CoV-2 关切变异株中,Delta 是最具毒性的,导致感染人群出现严重症状和死亡率增加。我们的研究旨在探讨 Delta 变异株的生物物理参数与临床观察结果之间的相关性。受体结合域(RBD)是与人类宿主细胞的第一个接触点,也是 Spike 蛋白的免疫显性形式。Delta 变异株 RBD 包含两个新突变 L452R 和 T478K。我们研究了单个突变和双突变对 RBD 在人 Expi293 细胞中的表达、尿素和热变性条件下 RBD 的稳定性以及 RBD 与血管紧张素转化酶 2(ACE2)受体和中和抗体的结合的影响,使用等温滴定量热法。与野生型 RBD 相比,Delta 变异株 RBD 显示出明显更高的表达水平,并且这种增加的表达归因于 L452R 突变。尽管它们是非保守的,但这些突变都没有显著影响 RBD 的结构和稳定性。所有突变体与 ACE2 和 Class 1 抗体(CC12.1 和 LY-CoV016)的结合亲和力与野生型相似。Delta 双突变体 L452R/T478K 与 Class 2 抗体(P2B-2F6 和 LY-CoV555)没有结合,与 Class 3 抗体(REGN10987)的结合能力弱了一百倍,而抗体结合能力的降低是由 L452R 突变决定的。这些结果表明,逃避中和抗体的免疫,而不是增加受体结合,是决定 Delta 变异株 RBD 适应性的主要生物物理参数。