Ribosomal Incorporation of Fluorosulfonyloxy-l-Phenylalanine into Macrocyclic Peptides for De Novo Target-Specific Covalent Binders
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Y Yang, P Liu, XY Cui, J Wu, W Cai…
Journal of the …, 2025
ACS Publications
Macrocyclic peptides are emerging as a promising molecular framework in covalent drug development due to their high specificity, affinity, and low toxicity, addressing challenges such as off-target effects and nonspecific binding associated with traditional covalent binders. Although mRNA display technology has advanced the discovery of covalent peptide binders, it has primarily focused on cysteine residues, thereby limiting the diversity of targetable proteins. In this study, we ribosomally incorporated 4-fluorosulfonyloxy-l …