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Cyclic peptides are at the forefront of efforts to pursue previously ‘undruggable’ therapeutic targets. Increasingly, researchers are adapting natural products and their biosynthetic systems to the preparation of cyclic peptide libraries. Alternatively, extant biotechnologies are being modified to increase the range and diversity of the compounds that they can access and incorporate into natural product motifs. A number of such systems have been validated with lead discovery and optimization against therapeutically relevant targets.
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