Therapeutic stapled peptides: Efficacy and molecular targets

Area of Science:

• Medicinal Chemistry
• Drug Discovery
• Biotechnology

Background:

• Peptide stapling stabilizes alpha-helical conformations, enhancing membrane permeability and proteolytic stability.
• Existing reviews cover stapling chemistries but lack a systematic summary of therapeutic stapled peptides for disease targets.

Purpose of the Study:

• To systematically review therapeutic stapled peptides, focusing on disease-related targets and development status.
• To highlight advances in peptide drug development using stapling technology.

Main Methods:

• Classification and analysis of stapled peptides based on receptor- and ligand-based design.
• Review of different stapling techniques, synthetic accessibility, and biological applicability.

Main Results:

• Stapled peptides show promise as therapeutic candidates for cancer, infectious diseases, inflammation, and diabetes.
• The technology facilitates the development of peptides with improved pharmacokinetic and biological properties.

Conclusions:

• Peptide stapling offers a robust strategy for developing next-generation peptide therapeutics.
• This review serves as a reference for designing stapled peptides against various diseases and targets.