Leonard Alison C, Weinstein Jonathan J, Steiner Paul J, Erbse Annette H, Fleishman Sarel J, Whitehead Timothy A
Department of Chemical and Biological Engineering, University of Colorado, Boulder, CO 80305, USA.
Department of Biomolecular Sciences, Weizmann Institute of Science, Rehovot, Israel.
bioRxiv. 2021 Nov 24:2021.11.22.469552. doi: 10.1101/2021.11.22.469552.
Stabilizing antigenic proteins as vaccine immunogens or diagnostic reagents is a stringent case of protein engineering and design as the exterior surface must maintain recognition by receptor(s) and antigen-specific antibodies at multiple distinct epitopes. This is a challenge, as stability-enhancing mutations must be focused on the protein core, whereas successful computational stabilization algorithms typically select mutations at solvent-facing positions. In this study we report the stabilization of SARS-CoV-2 Wuhan Hu-1 Spike receptor binding domain (S RBD) using a combination of deep mutational scanning and computational design, including the FuncLib algorithm. Our most successful design encodes I358F, Y365W, T430I, and I513L RBD mutations, maintains recognition by the receptor ACE2 and a panel of different anti-RBD monoclonal antibodies, is between 1-2°C more thermally stable than the original RBD using a thermal shift assay, and is less proteolytically sensitive to chymotrypsin and thermolysin than the original RBD. Our approach could be applied to the computational stabilization of a wide range of proteins without requiring detailed knowledge of active sites or binding epitopes, particularly powerful for cases when there are multiple or unknown binding sites.
将抗原蛋白稳定作为疫苗免疫原或诊断试剂是蛋白质工程与设计中的一个严格案例,因为其外表面必须在多个不同表位维持被受体和抗原特异性抗体识别的能力。这是一项挑战,因为增强稳定性的突变必须集中在蛋白质核心部位,而成功的计算稳定算法通常选择面向溶剂的位置进行突变。在本研究中,我们报告了使用包括FuncLib算法在内的深度突变扫描和计算设计相结合的方法来稳定新冠病毒武汉株Hu-1刺突蛋白受体结合域(S RBD)。我们最成功的设计编码了I358F、Y365W、T430I和I513L这几个RBD突变,维持了被受体ACE2以及一组不同的抗RBD单克隆抗体识别的能力,使用热位移分析显示其热稳定性比原始RBD高1至2摄氏度,并且比原始RBD对胰凝乳蛋白酶和嗜热菌蛋白酶的蛋白水解敏感性更低。我们的方法可应用于多种蛋白质的计算稳定,无需详细了解活性位点或结合表位,对于存在多个或未知结合位点的情况尤为有效。