Journal
CHEMICAL COMMUNICATIONS
Volume 52, Issue 29, Pages 5140-5143Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c6cc01226d
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Although small molecule covalent inhibitors have been widely explored, macromolecular covalent inhibitors are more difficult to design and implement. Here we present a strategy to enable a peptide to bind to its target protein covalently via proximity-enabled bio-reactivity, improving its activity of inhibiting the p53-Mdm4 interaction by 10-fold.
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