Kottani Rudresha, Valiulin Roman A, Kutateladze Andrei G
Department of Chemistry and Biochemistry, University of Denver, Denver, CO 80208-2436, USA.
Proc Natl Acad Sci U S A. 2006 Sep 19;103(38):13917-21. doi: 10.1073/pnas.0606380103. Epub 2006 Sep 6.
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.
溶液相组合化学在现代药物发现方面有着巨大的前景。非常需要直接方法来检测此类文库与生物靶点的结合情况。基于外部敏化的光不稳定标签的条件光释放，已开发出一种用于溶液相文库编码和筛选的方法。只有当配体与配备电子转移敏化剂的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。对释放到溶液中的标签进行分析，可揭示先导配体的身份或缩小潜在先导物的范围。
