Department of Cancer Immunology & Virology, Dana-Farber Cancer Institute, Boston, MA 02215, USA.
Department of Medicine, Harvard Medical School, Boston, MA 02115, USA.
Protein Eng Des Sel. 2023 Jan 21;36. doi: 10.1093/protein/gzad008.
Monoclonal antibody (mAb) therapies have rapidly become a powerful class of therapeutics with applications covering a diverse range of clinical indications. Though most widely used for the treatment of cancer, mAbs are also playing an increasing role in the defense of viral infections, most recently with palivizumab for prevention and treatment of severe RSV infections in neonatal and pediatric populations. In addition, during the COVID-19 pandemic, mAbs provided a bridge to the rollout of vaccines; however, their continued role as a therapeutic option for those at greatest risk of severe disease has become limited due to the emergence of neutralization resistant Omicron variants. Although there are many techniques for the identification of mAbs, including single B cell cloning and immunization of genetically engineered mice, the low cost, rapid throughput and technological simplicity of antibody phage display has led to its widespread adoption in mAb discovery efforts. Here we used our 27-billion-member naïve single-chain antibody (scFv) phage library to identify a panel of neutralizing anti-SARS-CoV-2 scFvs targeting diverse epitopes on the receptor binding domain (RBD). Although typically a routine process, we found that upon conversion to IgG, a number of our most potent clones failed to maintain their neutralization potency. Kinetic measurements confirmed similar affinity to the RBD; however, mechanistic studies provide evidence that the loss of neutralization is a result of structural limitations likely arising from initial choice of panning antigen. Thus this work highlights a risk of scFv-phage panning to mAb conversion and the importance of initial antigen selection.
单克隆抗体 (mAb) 疗法迅速成为一类强大的治疗药物,应用范围广泛,涵盖了多种临床适应症。尽管 mAb 最常用于治疗癌症,但它们在预防和治疗新生儿和儿科人群严重 RSV 感染方面,也在发挥着越来越大的作用。此外,在 COVID-19 大流行期间,mAb 为疫苗的推广提供了一个桥梁;然而,由于中和耐药的奥密克戎变体的出现,它们作为高危人群严重疾病治疗选择的持续作用已变得有限。虽然有许多鉴定 mAb 的技术,包括单个 B 细胞克隆和基因工程小鼠免疫,但抗体噬菌体展示的低成本、高通量和技术简单性导致其在 mAb 发现工作中得到广泛采用。在这里,我们使用了我们 270 亿成员的原始单链抗体 (scFv) 噬菌体文库来鉴定一组针对受体结合域 (RBD) 上不同表位的中和抗 SARS-CoV-2 scFv。尽管这通常是一个常规过程,但我们发现,在转化为 IgG 时,我们的许多最有效克隆未能保持其中和效力。动力学测量证实了与 RBD 的相似亲和力;然而,机制研究提供了证据,表明中和作用的丧失是由于初始筛选抗原选择引起的结构限制造成的。因此,这项工作强调了 scFv-噬菌体筛选到 mAb 转化的风险,以及初始抗原选择的重要性。