Strategies for Fine-Tuning the Conformations of Cyclic Peptides
Rasha Saad Jwad, Daniel Weissberger, Luke Hunter
Abstract
Cyclic peptides are promising scaffolds for drug development, attributable in part to their increased conformational order compared to linear peptides. However, when optimizing the target-binding or pharmacokinetic properties of cyclic peptides, it is frequently necessary to "fine-tune" their conformations, e.g., by imposing greater rigidity, by subtly altering certain side chain vectors, or by adjusting the global shape of the macrocycle. This review systematically examines the various types of structural modifications that can be made to cyclic peptides in order to achieve such conformational control.
Topics & Concepts
ChemistryCyclic peptideRigidity (electromagnetism)BiophysicsPeptideCombinatorial chemistryStereochemistryBiochemistryEngineeringStructural engineeringBiologyChemical Synthesis and AnalysisBiochemical and Structural CharacterizationCarbohydrate Chemistry and Synthesis