Jörg Scheuermann; Yuichi Onda; Gabriele Bassi; Abdullah Elsayed; Franziska Ulrich; Sebastian Oehler; Louise Plais; Dario Neri
Chem. Eur. J., 2021, 27(24), 7160-7167
https://doi.org/10.1002/chem.202005423

Abstract

We describe the synthesis and characterization of a novel DNA-encoded library of macrocyclic peptide derivatives, based on three sets of proteinogenic and non-proteinogenic amino acid building blocks and featuring the use of copper alkyne-azide cycloaddition (CuAAC) reaction for ring closure. The library (termed YO-DEL) which contains 1,254,838 compounds, was encoded with DNA in single-stranded format and was screened against target proteins of interest using affinity capture procedures and photocrosslinking. YO-DEL selections yielded specific binders against serum albumins, carbonic anhydrases and NKp46, a marker of activated Natural Killer cells.