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Achieving Skeletal Diversity in Peptide Macrocycles through The Use of Heterocyclic Grafts
Author(s) -
Kaldas Sherif J.,
Yudin Andrei K.
Publication year - 2018
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.201705418
Subject(s) - lability , peptide , cyclic peptide , combinatorial chemistry , chemistry , amino acid , biophysics , biochemistry , stereochemistry , computational biology , biology
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.