非免疫球蛋白配体药物应用进展

同抗体药物相比,非免疫球蛋白配体药物(Non-immunoglobulin scaffolds,非免蛋白配体药物)具有分子量小,不需要翻译后修饰,通常缺乏二硫键,并可进行直接的多聚化修饰等优点。最近几年,研发的非免蛋白配体药物种类就达到了二十余种,如Adhirons,Alphabodies,Centyrins,Pronectins,Repebodies,Affimers,和Obodies等,其中的139个非免疫球蛋白配体,可以特异靶向结合102种蛋白。这些非免疫球蛋白配体多用于癌症和炎症性疾病的治疗和诊断,其中有10多种非免疫球蛋白配体已经进入临床试验研究。最近,非免蛋白配体也被用于伴侣蛋白作结构解析研究,翻译后修饰的细胞内监控,或作为显微镜,流式细胞仪,Western印迹法等检测方法中抗体的替代品。

Progress in the Application of Non-immunoglobulin Scaffolds

Compared with the antibody drugs, the non-immune globulin scaffolds with a small molecular weight, do not need to be modified after translation, usually lack disulfide bonds, and can undergo straightforward multimerization. In recent years, the development of non-immune globulin scaffolds have reached more than 20 different types, such as Adhirons, Alphabodies, Centyrins, Pronectins, Repebodies, Affimers, and Obodies. 102 proteins have been specifically targeted by 139 different non-Ig scaffold binders. These non-immune globulin scaffolds are used for the treatment and diagnosis of cancer and inflammatory diseases, and there are more than 10 types of non-immune globulin scaffolds have been used in clinical trials. Recently, non-immune globulin scaffolds have also been used in research as structure determination chaperones, which are used in the study for intracellular monitoring of post-translational modifications or as an alternative to antibodiesfor microscopy, flow cytometry, and Western blotting, and so on.