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Hydrocarbon Stapling

Meaning

Hydrocarbon Stapling is a specialized chemical modification technique used in peptide drug design, where a hydrocarbon chain is introduced to cross-link or “staple” two non-adjacent amino acid side chains within a peptide sequence. This structural modification constrains the peptide into its biologically active alpha-helical conformation, which is often transient and unstable in its native state. The technique is used primarily to improve cell permeability and enhance resistance to rapid enzymatic degradation in vivo.