Amino Acids for Stapled Peptide
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Amino Acids for Stapled Peptide

Product List

BOC Sciences provides various amino acids for stapled peptides. You can find the right product for your project development in our list. If the product you need is not in the list, please contact us for custom amino acids.

What are Amino Acids for Stapled Peptides?

Amino acids for stapled peptide are a special class of non-natural amino acids, usually containing α -methyl and α -alkene groups. The olefin redecomposition reaction occurs between these two kinds of non-natural amino acids, cyclizing to form stable α -helix conformation of all carbon scaffold, and then synthesizing stapled peptide. Amino acids for stapled peptide have the characteristics of strong site specificity, wide range of substrates, small disturbance to protein structure and flexible use.

The formation of stable helical structures in peptide chains can be achieved through the ligation of amino acids. The selection and design of amino acids are aimed at incorporating stable cross-bridges into the peptide chain, thereby augmenting the stability and biological efficacy of the stapled peptide. By carefully choosing and combining these amino acids, it is possible to control the structure or characteristics of stapled peptides.

Example of peptide stapling.Fig.1 Example of peptide stapling. (Moiola et al., 2019)

Characteristics of Amino Acids for Stapled Peptides

  • Rigid Linkage

Amino acids used to form side-chain cross-bridges typically have a rigid connector structure that maintains the secondary structure of the peptide chain.

  • Enzyme Degradation Resistance

Amino acids selected should have high resistance to enzymatic degradation to increase the stability and half-life of the stapled peptide.

  • Cell permeability

Some specific amino acids can enhance the cell permeability of the stapled peptide, allowing it to enter the cell interior more efficiently.

  • Biological Activity

Amino acid selection for stapled peptides should take into account the structure and interaction sites of the target protein to ensure that the stapled peptide has high selectivity and affinity for the target protein.

Application of Amino Acids for Stapled Peptide

1. Application in genetic engineering

Amino acids for stapled peptide have many applications in genetic engineering drugs based on recombinant proteins, including recombinant cytokines, protein hormones, recombinant plasma proteins, recombinant thrombotic drugs, soluble receptors, therapeutic antibodies, recombinant medicinal plant and animal proteins, etc. Meanwhile, amino acids for stapled peptide can also be used in biological drugs and vaccines for prevention or therapy, nucleic acid drugs, small molecule polypeptide drugs, etc.

Amino acids for stapled peptide have more flexible and diverse R groups than other amino acids. Amino acids with different side chain pKa and REDOX potentials for stapled peptide can be used in kinetic studies. In addition, many amino acids for stapled peptide are used to detect protein-protein interactions due to their protein crosslinking properties.

2. Application in biology and medicine

Because amino acids for stapled peptide have the ability to insert proteins precisely, it makes it possible for scientists to manipulate the structure of large molecules of drugs as precisely as they do in small molecules. This shows that amino acids for stapled peptide have great application prospect in bio-medicine.

For example, amino acids for stapled peptide are bioorthogonal, improving the targeting specificity and efficacy of drugs. Proteins containing amino acids for stapled peptide (e.g. cytokines, growth factors, antibodies) are specifically linked to other modules to form pegylated proteins, antibody-drug conjugates, antibody-antisense oligonucleotide conjugates, bi-specific antibodies, etc.

Incorporating amino acids for stapled peptide into protein sequences is a strategy for designing new proteins in synthetic biology. This strategy is important for studying the folding and function of natural proteins. In addition, amino acids for stapled peptide are also widely used as initial modular building units in the total synthesis of natural products.

3. Application in pharmacy

Amino acids for stapled peptide are also important drugs in their own right, and they are important structural units of many commercially available drugs. Amino acids for stapled peptide are widely used in anti-bacterial, anti-inflammatory, anti-convulsant, anti-cell growth and anti-tumor drugs, and most of these drugs have entered clinical studies. For pharmaceutical companies, no one can ignore the role of amino acids for stapled peptide in the development of new drugs.


  1. Moiola M, et al. Stapled peptides-a useful improvement for peptide-based drugs[J]. Molecules, 2019, 24(20): 3654.
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