Stapled Peptide SynthesisPharmaceutical InformationUpdated on Jan 14, 2019 View more like this | Visit SHIRLEY, NY | Contact Cathy Miller |
What is stabled peptide
Stapled peptide is a full-carbon scaffold with an α-helical structure. The all-carbon scaffold stabilizes the α-helical structure, enhances the interaction between the peptide molecule and the protein, and the peptide can pass through the cell membrane and is not easily hydrolyzed. Stapled peptides have higher physiological activity than previous small molecule drugs and protein analogs.
Advantages of Custom Stapled Peptides
• Better target affinity
• Increased proteolytic resistance and serum half- life
• Increased cell permeability
• Targeting of either extracellular or intracellular proteins
• Non-immunogenicity
• Viable pharmacokinetics and in vivo stability
Synthesis Strategy
The synthesis of stapled peptides is different from that of a common peptide. By use of solid phase methods, the peptide chain is introduced two unnatural amino acids containing an α-methyl group and an α-alkenyl group, and then an olefin metathesis reaction occurs between two unnatural amino acids to constitutes a stable α-helical conformation.
Stapled peptide is a full-carbon scaffold with an α-helical structure. The all-carbon scaffold stabilizes the α-helical structure, enhances the interaction between the peptide molecule and the protein, and the peptide can pass through the cell membrane and is not easily hydrolyzed. Stapled peptides have higher physiological activity than previous small molecule drugs and protein analogs.
Advantages of Custom Stapled Peptides
• Better target affinity
• Increased proteolytic resistance and serum half- life
• Increased cell permeability
• Targeting of either extracellular or intracellular proteins
• Non-immunogenicity
• Viable pharmacokinetics and in vivo stability
Synthesis Strategy
The synthesis of stapled peptides is different from that of a common peptide. By use of solid phase methods, the peptide chain is introduced two unnatural amino acids containing an α-methyl group and an α-alkenyl group, and then an olefin metathesis reaction occurs between two unnatural amino acids to constitutes a stable α-helical conformation.
