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Designing stapled peptides to inhibit <scp>protein‐protein</scp> interactions: An analysis of successes in a rapidly changing field

Marie T. J. Bluntzer, James P. O’Connell, Terry Baker, Julien Michel, Alison N. Hulme

2020Peptide Science54 citationsDOIOpen Access PDF

Abstract

Abstract Two decades after their discovery, stapled peptide methodologies have evolved to a point where they can be used with confidence to generate therapeutic leads. Research groups across the world are testing innovative methodologies for their design, with dozens of publications released every month. A number of stapled peptide drug candidates have recently entered clinical trials. In this review, we provide an overview of successful methods for their construction, highlight trends in the deposited crystal structures of stapled peptide complexed to their targets and discuss properties that contribute towards improved pharmacological profiles.

Topics & Concepts

PeptideComputational biologyField (mathematics)Drug discoveryComputer scienceNanotechnologyCombinatorial chemistryData scienceChemistryBioinformaticsBiologyBiochemistryMaterials scienceMathematicsPure mathematicsChemical Synthesis and AnalysisMonoclonal and Polyclonal Antibodies ResearchRNA and protein synthesis mechanisms