Hook K Delaney, Chambers John T, Hili Ryan
Department of Chemistry , University of Georgia , Athens , GA 30602 , USA . Email:
Department of Chemistry , York University , Toronto , ON M3J 1P3 , Canada.
Chem Sci. 2017 Oct 1;8(10):7072-7076. doi: 10.1039/c7sc02779f. Epub 2017 Aug 21.
We have developed a novel high-throughput screening platform for the discovery of small-molecules catalysts for bond-forming reactions. The method employs an selection for bond-formation using amphiphilic DNA-encoded small molecules charged with reaction substrate, which enables selections to be conducted in a variety of organic or aqueous solvents. Using the amine-catalysed aldol reaction as a catalytic model and high-throughput DNA sequencing as a selection read-out, we demonstrate the 1200-fold enrichment of a known aldol catalyst from a library of 16.7-million uncompetitive library members.
我们开发了一种新型高通量筛选平台，用于发现用于形成键反应的小分子催化剂。该方法采用对负载反应底物的两亲性DNA编码小分子进行键形成的筛选，这使得筛选能够在各种有机溶剂或水性溶剂中进行。以胺催化的羟醛缩合反应作为催化模型，高通量DNA测序作为筛选读数，我们展示了从一个包含1670万个非竞争性文库成员的文库中，一种已知羟醛缩合催化剂实现了1200倍的富集。
