CRT Discovery Laboratories, Department of Crystallography, Birkbeck College, University of London, Malet Street, London, WC1E 7HX.
Anticancer Agents Med Chem. 2012 Jan;12(1):40-8. doi: 10.2174/187152012798764660.
Over the past decade, fragment-based drug discovery has developed significantly and has gained increasing popularity in the pharmaceutical industry as a powerful alternative and complement to traditional high-throughput screening approaches for hit identification. Fragment-based methods are capable of rapidly identifying starting points for structure-based drug design from relatively small libraries of low molecular weight compounds. The main constraints are the need for sensitive methods that can reliably detect the typically weak interactions between fragments and the target protein, and strategies for transforming fragments into higher molecular weight drug candidates. This approach has recently been validated as series of compounds from various programs have entered clinical trials.
在过去的十年中，基于片段的药物发现技术有了显著的发展，并在制药行业中越来越受欢迎，成为传统高通量筛选方法的有力替代和补充，可用于发现命中药物。基于片段的方法能够从相对较小的低分子量化合物文库中快速识别基于结构的药物设计的起点。主要的限制因素是需要灵敏的方法，能够可靠地检测片段与靶蛋白之间通常较弱的相互作用，以及将片段转化为更高分子量的候选药物的策略。这种方法最近已经得到了验证，因为来自各种项目的一系列化合物已经进入临床试验。
