A DNA-Encoded Chemical Library Based on Peptide Macrocycles.
Yuichi Onda, Gabriele Bassi, Abdullah Elsayed, Franziska Ulrich, Sebastian Oehler, Louise Plais, Jörg Scheuermann, Dario Neri
Chemistry (Weinheim an der Bergstrasse, Germany) 2021 Apr 26The synthesis and characterization of a novel DNA-encoded library of macrocyclic peptide derivatives are described; the macrocycles are based on three sets of proteinogenic and non-proteinogenic amino acid building blocks and featuring the use of copper(I)-catalyzed 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. © 2021 Wiley-VCH GmbH.
Citation
Yuichi Onda, Gabriele Bassi, Abdullah Elsayed, Franziska Ulrich, Sebastian Oehler, Louise Plais, Jörg Scheuermann, Dario Neri. A DNA-Encoded Chemical Library Based on Peptide Macrocycles. Chemistry (Weinheim an der Bergstrasse, Germany). 2021 Apr 26;27(24):7160-7167
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PMID: 33586277
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