Ribosomal incorporation of N-acetyl-3, 5-bis (chloromethyl) benzylthio-l-alanine for developing an mRNA-displayed bicyclic peptide library cyclized via 1, 3, 5-tris …
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M Li, H Yu, J Cheng, W Cai, Y Zhang…
Organic & Biomolecular …, 2025
pubs.rsc.org
We report a novel method for constructing an mRNA-displayed bicyclic peptide library cyclized through 1, 3, 5-tris (methyl) benzene by ribosomally incorporating N-acetyl-3, 5-bis (chloromethyl) benzylthio-L-alanine, enabling the selection of bicyclic peptides against specific targets. Using this method, we successfully identified bicyclic peptides that bind to human Trop2 and VEGF165, providing a new strategy for selecting bicyclic peptides cyclized by trimethylbenzene.
