Peptides Containing β-Amino Acid Patterns: Challenges and Successes in Medicinal Chemistry

The construction of bioactive peptides using beta-amino acid-containing sequence patterns is a very promising strategy to obtain analogues that exhibit properties of high interest for medicinal chemistry applications. beta-Amino acids have been shown to modulate the conformation, dynamics, and proteolytic susceptibility of native peptides. They can be either combined with alpha-amino acids by following specific patterns, which results in backbone architectures with well-defined orientations of the side chain functional groups, or assembled in de novo-designed bioactive beta- or alpha,beta-peptidic sequences. Such peptides display various biological functions, including antimicrobial activity, inhibition of proteinprotein interactions, agonism/antagonism of GPCR ligands, and anti-angiogenic activity.