Cell-Based Kinetic Target-Guided Synthesis of an Enzyme Inhibitor
Cell-Based Kinetic Target-Guided Synthesis of an Enzyme Inhibitor
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DOI：
10.1021/acsmedchemlett.7b00535
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发表时间：
2018-04-01
影响因子：
4.2
通讯作者：
Sellstedt, Magnus
中科院分区：
文献类型：
--
作者：
Antti, Henrik;Sellstedt, Magnus
Finding a new drug candidate for a selected target is an expensive and time-consuming process. Target guided-synthesis, or in situ click chemistry, is a concept where the drug target is used to template the formation of its own inhibitors from reactive building blocks. This could simplify the identification of drug candidates. However, with the exception of one example of an RNA-target, target-guided synthesis has always employed purified targets. This limits the number of targets that can be screened by the method. By applying methods from the field of metabolomics, we demonstrate that target-guided synthesis with protein targets also can be performed directly in cell-based systems. These methods offer new possibilities to conduct screening for drug candidates of difficult protein targets in cellular environments.
