Evaluation of on-resin head-to-tail cyclization protocols of peptides using automated peptide synthesizers

Peptide drug discovery programs have advanced to the clinic as the rules for small molecule-like transport and bioavailability have become more thoroughly understood. Macrocyclic peptides, in particular, have emerged as an extension to current peptide-based drug modalities of interest to the pharmacological community. Because macrocycles are structurally more rigid, improvements in specificity, stability and bioavailability are observed when compared to traditional linear peptide therapeutics.

Literature number: P256