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Synthesis and Screening of A DNA-Encoded Library of Non-Peptidic Macrocycles
preprintsubmitted on 27.12.2020, 15:54 and posted on 29.12.2020, 08:04 by Eric Koesema, Animesh Roy, Nicholas G. Paciaroni, Thomas Kodadek
There is considerable interest in the development of libraries of non-peptidic macrocycles as a source of ligands for difficult targets. We report here the solid-phase synthesis of a DNA-encoded library of several hundred thousand thioether-linked macrocycles. The library was designed to be highly diverse with respect to backbone scaffold diversity and to minimize the number of amide N-H bonds, which compromise cell permeability. The utility of the library as a source of protein ligands is demonstrated through the isolation of compounds that bind streptavidin, a model target, with high affinity.