New Drug Development Center (NDDC), Daegu-Gyeongbuk Medical Innovation Foundation (DGMIF), 80 Cheombok-ro, Dong-gu, Daegu 41061, Korea.
Department of Chemistry and Green-Nano Materials Research Center, Kyungpook National University, Daegu 41566, Korea.
J Med Chem. 2020 Jul 9;63(13):6578-6599. doi: 10.1021/acs.jmedchem.9b01782. Epub 2020 Feb 19.
DNA-encoded library technology (DELT) was introduced to our medicinal chemistry society more than 20 years ago. The application of DELT in the development of clinical candidates has been actively reported in the literature recently. A few representative examples include RIP1K inhibitors for inflammatory diseases and sEH inhibitors for endothelial dysfunction or abnormal tissue repair, among many others. Here, the authors would like to recall the recent developments in on-DNA synthetic methodologies for DEL construction and to analyze recent examples in the literature of DELT-based drug development efforts pursued in both the academic and industrial sectors. With this perspective, we hope to provide a useful summary of recent DELT-based drug discovery research and to discuss the future scope of DELT in medicinal chemistry.
DNA 编码库技术（DELT）在 20 多年前被引入我们的药物化学界。最近，文献中也积极报道了 DELT 在临床候选药物开发中的应用。其中有一些代表性的例子，包括用于炎症性疾病的 RIP1K 抑制剂和用于内皮功能障碍或异常组织修复的 sEH 抑制剂等。在这里，作者想要回顾一下最近在 DNA 合成方法学方面的进展，以分析文献中最近的基于 DELT 的药物开发工作的例子，这些工作是在学术界和工业界中进行的。通过这种视角，我们希望提供一个对最近基于 DELT 的药物发现研究的有用总结，并讨论 DELT 在药物化学中的未来范围。
