UCB, 216 Bath Road, Slough, SL1 4EN, UK.
Nat Rev Drug Discov. 2012 Jun 29;11(7):519-25. doi: 10.1038/nrd3756.
Although antibody-based therapeutics have become firmly established as medicines for serious diseases, the value of antibodies as tools in the early stages of small-molecule drug discovery is only beginning to be realized. In particular, antibodies may provide information to reduce risk in small-molecule drug discovery by enabling the validation of targets and by providing insights into the design of small-molecule screening assays. Moreover, antibodies can act as guides in the quest for small molecules that have the ability to modulate protein-protein interactions, which have traditionally only been considered to be tractable targets for biological drugs. The development of small molecules that have similar therapeutic effects to current biologics has the potential to benefit a broader range of patients at earlier stages of disease.
尽管抗体类药物已经成为治疗严重疾病的重要药物，但抗体作为小分子药物发现早期阶段的工具的价值才刚刚开始被认识到。特别是，抗体可以通过验证靶标并提供小分子筛选测定设计的见解，为降低小分子药物发现的风险提供信息。此外，抗体可以作为小分子的先导化合物，这些小分子能够调节蛋白质-蛋白质相互作用，这些相互作用传统上仅被认为是生物药物的可治疗靶点。开发具有与现有生物制剂相似治疗效果的小分子药物有可能使更广泛的疾病早期患者受益。
