Ding Yun, Franklin G Joseph, DeLorey Jennifer L, Centrella Paolo A, Mataruse Sibongile, Clark Matthew A, Skinner Steven R, Belyanskaya Svetlana
GlaxoSmithKline , Platform Technology & Science, ELT-Boston, 830 Winter Street, Waltham, Massachusetts 02451, United States.
ACS Comb Sci. 2016 Oct 10;18(10):625-629. doi: 10.1021/acscombsci.6b00078. Epub 2016 Sep 1.
DNA-encoded library technology (ELT) is a powerful tool for the discovery of new small-molecule ligands to various protein targets. Here we report the design and synthesis of biaryl DNA-encoded libraries based on the scaffold of 5-formyl 3-iodobenzoic acid. Three reactions on DNA template, acylation, Suzuki-Miyaura coupling and reductive amination, were applied in the library synthesis. The three cycle library of 3.5 million diversity has delivered potent hits for phosphoinositide 3-kinase α (PI3Kα).
DNA编码文库技术（ELT）是发现针对各种蛋白质靶点的新型小分子配体的强大工具。在此，我们报告基于5-甲酰基-3-碘苯甲酸支架的联芳基DNA编码文库的设计与合成。文库合成中应用了DNA模板上的三个反应，即酰化、铃木-宫浦偶联和还原胺化。具有350万种多样性的三轮文库已筛选出针对磷酸肌醇3-激酶α（PI3Kα）的有效命中化合物。
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