Bascom Palmer Eye Institute, Department of Ophthalmology, University of Miami School of Medicine, Miami, FL, USA.
Department of Pharmaceutical Sciences, North Texas Eye Research Institute, University of North Texas Health Science Center, Fort Worth, TX, USA.
Drug Discov Today. 2018 Mar;23(3):636-643. doi: 10.1016/j.drudis.2018.01.013. Epub 2018 Jan 8.
As productivity of pharmaceutical research and development (R&D) for small-molecule drugs declines, the trend in drug discovery strategies is shifting towards biologics, which predominantly target secreted or cell surface proteins. Receptors and ligands are the most-valuable drug targets. In contrast to conventional approaches of discovering one ligand at a time, the emerging technology of ligandomics can systematically map disease-selective cellular ligands in the absence of molecular probes. Biologics targeting these ligands with disease selectivity have the advantages of high efficacy, minimal adverse effects, wide therapeutic indices, and low safety-related attrition rates. Therefore, ligandomics represents a paradigm shift to address the bottleneck of target discovery for biologics development.
随着小分子药物的药物研发（R&D）生产力的下降，药物发现策略的趋势正在转向生物制剂，这些生物制剂主要针对分泌蛋白或细胞表面蛋白。受体和配体是最有价值的药物靶点。与传统的一次发现一种配体的方法相比，新兴的配体组学技术可以在没有分子探针的情况下系统地绘制疾病选择性细胞配体图谱。针对这些具有疾病选择性的配体的生物制剂具有高效、最小副作用、宽治疗指数和低安全性相关淘汰率的优点。因此，配体组学代表了一种范式转变，旨在解决生物制剂开发中目标发现的瓶颈问题。
