2023
DOI: 10.26434/chemrxiv-2023-xglb4-v2
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Peptidomimetic inhibitors of β-strand mediated protein-protein interactions: tuning binding affinity of intrinsically disordered sequences by covalent backbone modification

Emma Cawood,
Emily Baker,
Thomas Edwards
et al.

Abstract: A significant challenge for chemical biology is to develop methods that enable targeting of protein-protein interactions (PPIs). Given that many PPIs involve a folded protein domain and a peptide that is intrinsically disordered in isolation, peptides present potential starting points for designing PPI modulators. Using the interaction between small ubiquitin-like modifiers (SUMO) and SUMO-interacting motifs (SIMs), here we show that N-methylation of the peptide backbone can effectively restrict accessible pep… Show more

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