Cyclic peptides: backbone rigidification and capability of mimicking motifs at protein-protein interfaces.

ABSTRACT: Cyclization is commonly employed in efforts to improve the target binding affinity of peptide-based probes and therapeutics. Many structural motifs have been identified at protein-protein interfaces and provide promising targets for inhibitor design using cyclic peptides. Cyclized peptides are generally assumed to be rigidified relative to their linear counterparts. This rigidification potentially pre-organizes the molecules to interact properly with their targets. However, the actual impact of cyclization on, for example, peptide configurational entropy, is currently poorly understood in terms of both its magnitude and molecular-level origins. Moreover, even with thousands of desired structural motifs at hand, it is currently not possible to a priori identify the ones that are most promis

SUBMITTER: Huang H 

PROVIDER: S-EPMC7790991 | biostudies-literature | 2021 Jan

REPOSITORIES: biostudies-literature