小分子药物筛选技术研究现状及其应用进展  

Current Research Status and Application Technical Progress of Small Molecule Drug Screening Technology

作　　者：武瑞君 李玮琦[1] 杨阳 王晶 张鑫 方子寒 张小奕 苏月[1] WU Ruijun;LI Weiqi;YANG Yang;WANG Jing;ZHANG Xin;FANG Zihan;ZHANG Xiaoyi;SU Yue(China National Center for Biotechnology Development,Beijing 100039,China)

机构地区：[1]中国生物技术发展中心,北京100039

出　　处：《医药导报》2024年第2期255-261,共7页Herald of Medicine

摘　　要：小分子药物筛选技术伴随着药物的发现正在不断更新和拓展,药物筛选技术的创新可以提高研发效率和成功率、缩短研发周期、降低成本。从基于已知活性化合物和高通量筛选等传统筛选技术,到基于结构的药物发现、基于片段的药物发现、DNA编码化合物库、蛋白降解靶向联合体等新技术,小分子药物筛选技术在不断拓宽小分子药物的市场潜力。该文将介绍目前小分子药物筛选技术整体现状,系统综述各技术及其优劣势,为小分子药物筛选新技术的发展提供重要参考。Small molecule drug screening technology is continuously evolving and expanding along with drug discovery,and the innovation in drug screening technology can improve the research and development efficiency and success rate,shorten the cycle time,and reduce the cost.From traditional screening technologies based on known active compounds and high-throughput screening(HTS)to new technologies such as structure-based drug discovery(SBDD),fragment-based drug discovery(FBDD),DNA encoded compound library(DEL)and proteolysis targeting chimeras(PROTAC),small molecule drug screening technologies are continuously broadening the market potential for small molecule drugs.This article will provide an overview of the current status of small molecule drug screening technology,systematically review each technique along with their advantages and disadvantages,and offer essential insights for the development of new small molecule drug screening technologies.

关 键 词：小分子药物筛选技术 高通量筛选 基于结构的药物发现 基于片段的药物发现 DNA编码化合物库 蛋白降解靶向联合体 

分 类 号：R945[医药卫生—微生物与生化药学]