Laboratoire de physique de l'Ecole normale supérieure, CNRS, PSL University, Sorbonne Université, Université Paris-Cité, Paris, France.
Italian Institute for Genomic Medicine, IRCCS Candiolo, Candiolo, Italy.
PLoS Comput Biol. 2024 Oct 14;20(10):e1012522. doi: 10.1371/journal.pcbi.1012522. eCollection 2024 Oct.
Exquisite binding specificity is essential for many protein functions but is difficult to engineer. Many biotechnological or biomedical applications require the discrimination of very similar ligands, which poses the challenge of designing protein sequences with highly specific binding profiles. Experimental methods for generating specific binders rely on in vitro selection, which is limited in terms of library size and control over specificity profiles. Additional control was recently demonstrated through high-throughput sequencing and downstream computational analysis. Here we follow such an approach to demonstrate the design of specific antibodies beyond those probed experimentally. We do so in a context where very similar epitopes need to be discriminated, and where these epitopes cannot be experimentally dissociated from other epitopes present in the selection. Our approach involves the identification of different binding modes, each associated with a particular ligand against which the antibodies are either selected or not. Using data from phage display experiments, we show that the model successfully disentangles these modes, even when they are associated with chemically very similar ligands. Additionally, we demonstrate and validate experimentally the computational design of antibodies with customized specificity profiles, either with specific high affinity for a particular target ligand, or with cross-specificity for multiple target ligands. Overall, our results showcase the potential of leveraging a biophysical model learned from selections against multiple ligands to design proteins with tailored specificity, with applications to protein engineering extending beyond the design of antibodies.
精致的结合特异性对于许多蛋白质功能至关重要,但很难进行工程设计。许多生物技术或生物医学应用都需要区分非常相似的配体,这就需要设计具有高度特异性结合特性的蛋白质序列。用于生成特异性配体的实验方法依赖于体外选择,这种方法在文库大小和特异性谱控制方面存在局限性。最近通过高通量测序和下游计算分析证明了额外的控制。在这里,我们采用这种方法来证明特定抗体的设计超出了实验所探测的范围。我们在一个需要区分非常相似的表位的背景下这样做,而这些表位不能通过实验从选择中存在的其他表位中分离出来。我们的方法涉及到识别不同的结合模式,每种模式都与一种特定的配体相关联,针对这些配体,抗体要么被选择,要么不被选择。利用噬菌体展示实验的数据,我们表明,即使这些模式与化学性质非常相似的配体相关联,该模型也能成功地将这些模式分离出来。此外,我们还通过实验验证了具有定制特异性特征的抗体的计算设计,这些抗体要么对特定的目标配体具有特异性高亲和力,要么对多个目标配体具有交叉特异性。总的来说,我们的结果展示了利用从多种配体的选择中学习到的生物物理模型来设计具有定制特异性的蛋白质的潜力,这种方法在蛋白质工程中的应用超出了抗体设计的范围。