Selection of DNA-Encoded Small Molecule Libraries Against Unmodified and Non-Immobilized Protein Targets

Selection of DNA-Encoded Small Molecule Libraries Against Unmodified and Non-Immobilized Protein Targets
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DOI:
10.1002/anie.201404830
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发表时间:
2014-09-15
影响因子:
16.6
通讯作者:
Li, Xiaoyu
Li, Xiaoyu
中科院分区:
化学1区
文献类型:
--
作者:
Zhao, Peng;Chen, Zitian;Li, Xiaoyu

文献摘要

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针对生物靶标的DNA编码文库的选择已经成为化学生物学和药物发现中的重要发现方法,但是需要修饰和固定的靶标仍然是一个显著的缺点。利用末端保护策略和配体诱导的光交联,我们证明了DNA编码文库的迭代选择可以用未修饰的和非固定化的蛋白质靶来实现。
The selection of DNA-encoded libraries against biological targets has become an important discovery method in chemical biology and drug discovery, but the requirement of modified and immobilized targets remains a significant disadvantage. With a terminal protection strategy and ligand-induced photo-crosslinking, we show that iterated selections of DNA-encoded libraries can be realized with unmodified and non-immobilized protein targets.