Macrocyclization strategies for cyclic peptides and peptidomimetics.

ABSTRACT: Peptides are a growing therapeutic class due to their unique spatial characteristics that can target traditionally "undruggable" protein-protein interactions and surfaces. Despite their advantages, peptides must overcome several key shortcomings to be considered as drug leads, including their high conformational flexibility and susceptibility to proteolytic cleavage. As a general approach for overcoming these challenges, macrocyclization of a linear peptide can usually improve these characteristics. Their synthetic accessibility makes peptide macrocycles very attractive, though traditional synthetic methods for macrocyclization can be challenging for peptides, especially for head-to-tail cyclization. This review provides an updated summary of the available macrocyclization chemistries, suc

SUBMITTER: Bechtler C 

PROVIDER: S-EPMC8372203 | biostudies-literature | 2021 Aug

REPOSITORIES: biostudies-literature