Scheuermann Jörg, Neri Dario
ETH Zurich, Department of Chemistry and Applied Biosciences, Institute of Pharmaceutical Sciences, 8093 Zurich, Switzerland.
Curr Opin Chem Biol. 2015 Jun;26:99-103. doi: 10.1016/j.cbpa.2015.02.021. Epub 2015 Mar 13.
In contrast to single-pharmacophore DNA-encoded libraries, where only one chemical moiety is linked to DNA, dual-pharmacophore DNA-encoded chemical libraries feature the display of two independent small-molecules in close proximity. This, in principle, allows to explore adjacent epitopes on a pharmaceutical target of choice and hence the discovery of simultaneously binding pairs of fragments, by virtue of the chelate effect.
与单药效团DNA编码文库（其中只有一个化学部分与DNA相连）不同，双药效团DNA编码化学文库的特点是在近距离展示两个独立的小分子。原则上，这允许探索所选药物靶点上相邻的表位，从而借助螯合效应发现片段的同时结合对。
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