Direct screening of solution phase combinatorial libraries encoded with externally sensitized photolabile tags
Direct screening of solution phase combinatorial libraries encoded with externally sensitized photolabile tags
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DOI：
10.1073/pnas.0606380103
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发表时间：
2006-09-19
影响因子：
11.1
通讯作者：
Kutateladze, Andrei G.
中科院分区：
文献类型：
--
作者：
Kottani, Rudresha;Valiulin, Roman A.;Kutateladze, Andrei G.
溶液相组合化学为现代药物发现带来了巨大的希望。非常需要的是直接的方法来测定这样的文库与生物靶标的结合。基于外部敏化的光不稳定标签的条件光释放，开发了一种编码和筛选溶液相库的方法。只有当配体和受体之间发生所需的结合事件时，编码标签才会释放到溶液中，并配备电子转移敏化剂。在溶液中分析释放的标签，从而揭示先导配体的身份或缩小潜在先导的范围。
Solution phase combinatorial chemistry holds an enormous promise for modern drug discovery. Much needed are direct methods to assay such libraries for binding of biological targets. An approach to encoding and screening of solution phase libraries has been developed based on the conditional photorelease of externally sensitized photolabile tags. The encoding tags are released into solution only when a sought-for binding event occurs between the ligand and the receptor, outfitted with an electron-transfer sensitizer. The released tags are analyzed in solution revealing the identity of the lead ligand or narrowing the range of potential leads.