3 years ago

Front Cover: Targeted Nanoswitchable Inhibitors of Protein–Protein Interactions Involved in Apoptosis (ChemMedChem 1/2019)

Laura Nevola, Monica Varese, Andrés Martín-Quirós, Giacomo Mari, Kay Eckelt, Pau Gorostiza, Ernest Giralt

Abstract

The Front Cover shows the concept of a generalized template design strategy to obtain light‐regulated peptide inhibitors of helix‐mediated protein–protein interactions (PPIs). Using the available information about hot spots at protein–peptide interfaces, we developed modular peptides containing a photoisomerizable crosslinker that provide reversible and reproducible photocontrol of the protein‐binding ability and the inhibitory activity of peptides. This effect can be imagined as different components of toy houses (peptide inhibitors) that are reassembled with light to be active or not. This approach has been validated in two important targets (Bcl‐xL‐Bak and MDM2‐p53) and could potentially be applied in a broad range of therapeutically relevant PPIs. More information can be found in the Full Paper by Pau Gorostiza, Ernest Giralt et al. on page 100 in Issue 1, 2019 (DOI: 10.1002/cmdc.201800647).

Publisher URL: https://onlinelibrary.wiley.com/doi/abs/10.1002/cmdc.201800799

DOI: 10.1002/cmdc.201800799

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