Fragment-to-Lead Medicinal Chemistry Publications in 2019
Fragment-to-Lead Medicinal Chemistry Publications in 2019
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DOI：
10.1021/acs.jmedchem.0c01608
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发表时间：
2020-12-24
影响因子：
7.3
通讯作者：
Urushima, Tatsuya
中科院分区：
文献类型：
--
作者：
Jahnke, Wolfgang;Erlanson, Daniel A.;Urushima, Tatsuya
基于片段的药物发现（FBDD）已经发展和成熟到一个点，它是有价值的跟踪其应用的程度和细节。本《视角》总结了2019年发布的成功的片段到线索故事。这是从2015年出版的文学作品开始的系列中的第五部。分析的筛选方法，优化策略，以及命中和线索的分子特性，希望通知FBDD的最佳实践。而且，FBDD还在不断发展，总结了最新的技术和新兴趋势。这些包括共价FBDD，用于蛋白质或蛋白质-蛋白质相互作用的稳定化的FBDD，用于酶激活剂的FBDD，新的筛选技术，以及库设计和化学合成的进展。
Fragment-based drug discovery (FBDD) has grown and matured to a point where it is valuable to keep track of its extent and details of application. This Perspective summarizes successful fragment-to-lead stories published in 2019. It is the fifth in a series that started with literature published in 2015. The analysis of screening methods, optimization strategies, and molecular properties of hits and leads are presented in the hope of informing best practices for FBDD. Moreover, FBDD is constantly evolving, and the latest technologies and emerging trends are summarized. These include covalent FBDD, FBDD for the stabilization of proteins or protein-protein interactions, FBDD for enzyme activators, new screening technologies, and advances in library design and chemical synthesis.