Synthesis and Screening of A DNA-Encoded Library of Non-Peptidic Macrocycles
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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.
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2019 ◽
pp. 183-194
2000 ◽
Vol 10
(24)
◽
pp. 2693-2696
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2003 ◽
Vol 68
(15)
◽
pp. 5805-5811
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2010 ◽
Vol 12
(3)
◽
pp. 321-326
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