Macrocyclic Iminopeptides Diversify To Better Target Proteins.
Leslie RegueraDaniel G RiveraPublished in: ChemMedChem (2020)
Among the many methods available for accessing conformationally diverse cyclic peptides, the derivatization of macrocyclic iminopeptides has remained notably underexplored. Now, a relevant complexity-generating method expands the repertoire of synthetic strategies exploiting the reactivity of an imino bond embedded in the cyclic peptide skeleton. Here we highlight a recent report describing the on-resin construction of a new family of macrocyclic peptide/natural product-inspired hybrids, namely "PepNats", by derivatization of cyclic iminopeptides through 1,3-cycloaddition reactions. A proof-of-concept with PepNats bearing peptide sequences that mimic protein hot loops demonstrated the potential of this strategy to create novel macrocyclic peptide ligands capable of modulating protein-protein interactions.
Keyphrases
- ms ms
- liquid chromatography tandem mass spectrometry
- high performance liquid chromatography
- gas chromatography mass spectrometry
- simultaneous determination
- signaling pathway
- tandem mass spectrometry
- amino acid
- gas chromatography
- mass spectrometry
- binding protein
- ultra high performance liquid chromatography
- protein protein