Exploring a Structural Data Mining Approach to Design Linkers for Head-to-Tail Peptide Cyclization.

ABSTRACT: Peptides have recently regained interest as therapeutic candidates, but their development remains confronted with several limitations including low bioavailability. Backbone head-to-tail cyclization, i.e., setting a covalent peptide bond linking the last amino acid with the first one, is one effective strategy of peptide-based drug design to stabilize the conformation of bioactive peptides while preserving peptide properties in terms of low toxicity, binding affinity, target selectivity, and preventing enzymatic degradation. Starting from an active peptide, it usually requires the design of a linker of a few amino acids to make it possible to cyclize the peptide, possibly preserving the conformation of the initial peptide and not affecting its activity. However, very little is known about

SUBMITTER: Karami Y 

PROVIDER: S-EPMC10599322 | biostudies-literature | 2023 Oct

REPOSITORIES: biostudies-literature