基于片段的药物发现(fragment-based drug discovery,FBDD)是基于结构的药物研发方法的延伸,正日趋成熟,并在药物研发中发挥着重要的作用。该方法是通过SPR、MS、NMR、X-ray等生物物理方法快速筛选片段分子库,检测并发现分子量小、相对结合效率高的活性化合物,继之结合结构生物学研究进行分子优化设计,得到更为类药的先导和候选化合物,进行创新性药物开发。与传统高通量筛选等方法相比,FBDD具有十分显著的优点,发现的活性片段利于优化、获得的活性分子成药性高。本文结合实例综述了基于片段的药物发现方法的研究进展。
【英文摘要】
As an extension of the structure-based drug discovery,fragment-based drug discovery is matured increasingly,and plays an important role in drug development.Fragments in a small library,with lower molecular mass and high ligand efficiency,are detected by SPR,MS,NMR,X-ray crystallography technologies and other biophysical methods.Then they are considered as starting points for chemical optimization with the guidance of structural biology methods to get good drug-like lead and candidate compounds.In this artic...
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