In Vitro Selection of Macrocyclic <scp>d</scp>/<scp>l</scp>-Hybrid Peptides against Human EGFR

d/l-Hybrid peptides are an attractive class of molecular modality because they able to exhibit high proteolytic stability and unique structural diversity which cannot be accessed by those consisting only proteinogenic l-amino acids. Despite such expectation, it has not been possible devise de novo d/l-hybrid capable disrupting the function a protein target(s) due lack effective method that reliably constructs highly diverse library screens active species. Here we report for first time construction 1012 members macrocyclic containing five kinds d-amino acids performance RaPID selection against human EGFR as showcase uncover PPI (protein–protein interaction) inhibitors.