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Cyclic peptides are an exciting class of compounds that are currently underexploited as chemical probes. Recent advances in peptide chemistry, screening and sequencing technologies have permitted the efficient generation and screening of natural product-like cyclic peptide libraries to identify high-affinity and -selectivity ligands against targets of interest, providing new opportunities for the development of chemical probes, including for challenging targets. This chapter reviews recent advances in cyclic peptide technologies and provides examples where cyclic peptides have been used to study the biology of their targets.

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