Cyclic Peptides in the Spotlight: New Technologies to Synthesize Your Dream Structures

As one of the most effective peptide modification strategies, cyclization imparts distinct biochemical and therapeutic properties to peptides for drug development, such as increased half-life and cell permeability. The fast-growing demand for diverse cyclic peptides in the field of drug discovery has significantly enhanced our capability and capacity for cyclic peptide production. In this webinar, we will discuss the latest pharmaceutical applications and share our industrial synthesis experience with various cyclic peptides, focusing on solutions to some notorious cyclization side reactions.

During the webinar, we will introduce several new technologies for synthesizing cyclic peptides. Disulfide bonds are typically formed through oxidation. However, addressing side reaction issues has been a persistent challenge. New methods to replace oxidation reagents have been developed and implemented in our labs. This new synthesis strategy has successfully improved cyclization efficiency. Additionally, we will introduce another technology for increasing capacity. Using this method, we can synthesize 1500-2000 Cys-Cys peptides per month, and we have launched the cyclic peptide library service. Furthermore, we have explored an alternative Cys protection group to synthesize Cys-Cys cyclic peptides with an additional free thiol group, greatly enhancing the design flexibility of cyclic peptides.

During the webinar, we will cover the following topics:

Advantages of cyclic peptides and their current market status

Key pharmaceutical applications of cyclic peptides

Strategies for addressing common side reactions in cyclization reactions

Introduction to the cyclic peptide library service

One-stop solution services and the cGMP capacity of Genscript .

In this webinar, you will learn

Webinar Details

  • Date: December 7th, 2023
  • Time: 10:30 AM SGT (GMT+8)
  • Speaker:
Dr. Mina Wang Dr. Mina Wang

Senior Peptide Scientist, R&D Department, GenScript Biotech

Dr. Mina Wang joined GenScript at the beginning of 2022 as a senior scientist in peptides. Before joining GenScript, she earned her Ph.D. in chemistry from the University of South Florida. Since joining GenScript, her work has been focused on establishing and updating the cyclic peptide service.

FAQs

  • Q&A

    1. Do you have a library of common cyclic peptides for peptide screening?

    • We exclusively offer customized cyclic peptide libraries. If you require assistance with library design, our robust AI peptide design team is ready to help.

    2. How does the prospect of using enzymes for peptide cyclization compare to chemical synthesis?

    • Advantages

      • Enzyme peptide cyclization is more eco-friendly.
      • In some situations, enzymes can cyclize short peptides and hydrophobic peptides, which are very difficult for chemical synthesis.
    • Disadvantages

      • Peptide sequences must meet certain limitations. For example, SurE can be used for head-to-tail cyclization, but it strictly requires the pairing of terminal amino acids with opposite configurations (i.e., L-amino acid at N-terminus and D-amino acid at C-terminus) and a preference for bulky aromatic/aliphatic residues at the terminal positions.
      • The purity of linear peptides usually needs to be high.

    3. Do you have experience with epimerization during peptide synthesis? If so, what do you usually do?

    • Several strategies can be applied:

      • Using conjugations with strong activity, like HATU;
      • Reduce the reaction time;
      • Lower the temperature at the activation step of amino acids.

    4. How is the prospect of lasso peptides from an industrial perspective?

    • Lasso peptides exhibit better stability than linear peptides and have been increasingly explored in the field of anti-infection. Many academic researchers have conducted extensive work in this area. However, in the industrial sector, the demand for lasso peptides is not significant. This might be attributed to the potentially high cost of synthesis and impurity studies.

    5. Please comment on the stability and synthesis cost of cyclic, bicyclic, and tricyclic compounds.

    • In my opinion, the stability of cyclic peptides has more to do with the cyclization strategies rather than the number of rings. For example, a thioether bond is much more stable than a disulfide bond, whether in vivo or in vitro, even when there are two disulfide bonds. Usually, the synthesis cost of these, arranged in increasing order, is cyclic peptide < bicyclic peptide < tricyclic peptide.

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