Achieving Skeletal Diversity in Peptide Macrocycles through The Use of Heterocyclic Grafts.
Sherif J KaldasAndrei K YudinPublished in: Chemistry (Weinheim an der Bergstrasse, Germany) (2018)
Despite their therapeutic potential, peptide macrocycles often suffer from drawbacks such as low membrane permeability, proteolytic instability, and conformational lability. As a result, there have been significant efforts to "depeptidize" amino acid-rich macrocycles through the incorporation of heterocyclic grafts into their backbones. In this concept article, we summarize selected recent methodologies that can be used to introduce heterocycles into cyclic peptides.