Macrocyclic imino-peptides diversify to better target proteins.

Macrocyclic imino-peptides diversify to better target proteins.
ChemMedChem. 2020 Jun 09;:
Authors: Rivera DG, Reguera L
Abstract
Among the many methods available for accessing conformationally diverse cyclic peptides, the derivatization of macrocyclic imino-peptides 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 imino-peptides using 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.
PMID: 32516501 [PubMed - as supplied by publisher]

Source: ChemMedChem - June 8, 2020 Category: Chemistry Authors: Rivera DG, Reguera L Tags: ChemMedChem Source Type: research