Passariello Margherita, Rapuano Lembo Rosa, Manna Lorenzo, Miele Ciro, Merlino Antonello, Mazzaccara Cristina, Leonardi Antonio, De Lorenzo Claudia
Ceinge-Biotecnologie Avanzate s.c.a.r.l., Via Gaetano Salvatore 486, 80145 Naples, Italy.
Department of Molecular Medicine and Medical Biotechnologies, University of Naples "Federico II", Via S. Pansini 5, 80131 Naples, Italy.
Int J Mol Sci. 2025 Mar 18;26(6):2721. doi: 10.3390/ijms26062721.
Cardiovascular diseases, including thrombosis, are the leading cause of mortality worldwide. The generation of monoclonal antibodies (mAb) targeting specific coagulation factors could provide more targeted and safer anticoagulant therapies. Factor V (FV) is a critical cofactor in the prothrombinase complex, which catalyzes the conversion of prothrombin to thrombin, a key enzyme in the coagulation cascade. We isolated a novel human antibody specific to FV by using phage display technology. The selection occurred by panning a large repertoire of phages expressing human antibody fragments (scFv) in parallel on the purified recombinant protein in its native form (FV) or activated by proteolytic maturation (Factor Va (FVa)). Through ELISA screening, we identified the clone with the highest binding affinity for both targets, and it was successfully converted into IgG1. The novel human mAb, called D9, was found capable of binding to Factor V with a low nM affinity both by ELISA and BLI assays, whereas its cross-reactivity with some other coagulation factors was found null or very poor. Furthermore, when tested in blood clotting tests, it was found able to prolong activated partial thromboplastin time (aPTT). Thus, D9 could become not only a potential therapeutic agent as a specific anticoagulant but also a precious tool for diagnostic and research applications.
包括血栓形成在内的心血管疾病是全球主要的死亡原因。生成靶向特定凝血因子的单克隆抗体(mAb)可为抗凝治疗提供更具针对性且更安全的方法。因子V(FV)是凝血酶原酶复合物中的关键辅因子,它催化凝血酶原转化为凝血酶,而凝血酶是凝血级联反应中的关键酶。我们利用噬菌体展示技术分离出了一种针对FV的新型人源抗体。筛选过程是通过在天然形式的纯化重组蛋白(FV)或经蛋白水解成熟激活的蛋白(因子Va(FVa))上平行淘选大量表达人抗体片段(scFv)的噬菌体文库来进行的。通过ELISA筛选,我们鉴定出了对两个靶点具有最高结合亲和力的克隆,并成功将其转化为IgG1。这种新型人源mAb名为D9,通过ELISA和BLI分析发现它能够以低纳摩尔亲和力结合因子V,而其与其他一些凝血因子的交叉反应性为零或非常低。此外,在凝血试验中测试时,发现它能够延长活化部分凝血活酶时间(aPTT)。因此,D9不仅可能成为一种作为特异性抗凝剂的潜在治疗药物,还可能成为诊断和研究应用中的宝贵工具。