Drug Design advanced
Peptide-Protein Stapling
Chemical stapling of peptides to proteins for enhanced stability, cell penetration, and target binding.
By Encyclopeptide Editorial | 1 min read
stapling protein stability cell-penetration therapeutic
Overview
Peptide-protein stapling involves covalently linking peptide segments to protein scaffolds to create constrained, stable chimeric molecules with enhanced therapeutic properties.
Stapling Approaches
Chemical Crosslinking
- Disulfide bonds
- Thioether bonds
- Click chemistry
Backbone Cyclization
- Head-to-tail cyclization
- Side-chain to side-chain
- Stapled secondary structures
Benefits
- Increased proteolytic stability
- Enhanced cell membrane penetration
- Pre-organized binding conformation
- Improved receptor selectivity
- Extended half-life
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