Cyclic Peptide Synthesis

Peptide cyclization is carried out on the backbone or side chain of the peptide. It not only eliminates the amino and carboxyl groups at the N-terminus and C-terminus of the peptide that are susceptible to degradation by exopeptidases, but also enables the peptide to maintain a conformation that is conducive to binding to the receptor, thereby greatly improving the biological activity of these peptides.

Cyclic Peptide Types

cyclo(X1-X2——–Xn) Head-to-tail cyclization	Diketopiperazine

X = NH : polypeptide X = O : depsipeptide (including N-methyl amino acids)	R=H : cyclo(X-Pro) R=OH : cyclo(X-Hyp)	cyclo(X-X)
Cyclization at side chain	Lactone/Thiolactone	Thioether

	X=O : lactone X=S : thiolactone
Deamino-dicarba

Stapled Peptides

Stapled peptides are modified peptides that usually have an α-helical conformation and are constrained by a synthetic scaffold (staple compound). Stapled peptides have a higher degree of α-helical conformation and significantly enhance their ability to bind to targets. They can penetrate cell membranes, are difficult to be hydrolyzed by proteases, and have a longer half-life in vivo.

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