Technology

PepDom™ Platform

A Versatile Route to Biologically Active Compounds

Why Develop Peptidomimetics?

The premise of all polypeptide drugs or therapies used for diagnosis and treatment is to first pass through the body barrier and then reach the target site accurately. However, no matter how the polypeptide acts on the human body, the stability and bioavailability of the polypeptide in the body are very poor, which leads to unsatisfactory results in some meaningful drug research or disease therapy development.

Fig. 1 De novo discovery of peptidomimetic affinity reagents for human angiotensin converting enzyme 2. (Zhang, et al., 2022)

It is of great interest to develop peptidomimetics that have the same biological effects as native peptides, but with enhanced properties such as higher proteolytic stability, higher bioavailability, and generally improved selectivity or potency. These advantages make it widely used in all aspects of biomedicine, especially the discovery of new drug candidates.

Our Technology

Relying on our technology, more stable and more bioavailable peptidomimetic compounds are developed for diversified research, thus enriching the treatment and diagnosis methods.

Unique Peptidomimetic Development Platform

PepDom™ is a unique peptidomimetic development platform based on three key technologies:

• Peptidomimetic Design Technology: At the DNA level, peptidomimetic sequences are designed to encode various functional amino acids, or to perform amino acid substitutions and additions or deletions in known sequences. The sequence is random and diversity is guaranteed.

• Peptidomimetic Discovery Technology: DNA sequence is transcribed into mRNA in vitro, the 3' end of mRNA is combined with puromycin through a linker, then translated to obtain a high-capacity peptidomimetic library, and then reverse transcribed to obtain nucleic acid-peptide complexes. Perform unrestricted screening, and finally amplify and enrich the DNA sequence of the target peptidomimetic.

• Peptidomimetic Modification Technology: As the optimization technology of PepDom™, peptidomimetic modification runs through the whole process of project development, usually involving overall and partial modification. Compared with ordinary peptides, modified peptidomimetics not only obtain high affinity for target proteins and Selective, but also more stable in vivo.

By combining these techniques, PepDom™ can identify target peptidomimetics faster than any other technique and optimize target peptidomimetics with unprecedented speed.

Fig. 2 Overview of mRNA display. (Sohrabi, et al., 2020)

What Can PepDom™ Do?

We have developed and continue to expand our toolbox to leverage ever-evolving cutting-edge technologies to drive continued innovation in our technology platform.

Discovery

PepDom™ works closely with customers around the world to develop peptidomimetic lead compounds for each target in disease areas and drug administration routes.

• Diabetes. At present, diabetes is the seventh leading cause of death in the United States, and more than 90% of diabetes patients have type 2 diabetes. The characteristic of type 2 diabetes is that insulin cannot be used correctly. At present, the biological treatment for diabetes patients usually focuses on injecting various insulin products, and there is no oral insulin preparation. It is speculated that oral treatment will reduce the side effects of insulin administration, such as weight gain and hypoglycemia.
  However, oral drugs, such as peptide ligands, are often difficult to reach the target completely because bioavailable peptides must pass through the intestinal mucosa to reach their target. Our technology has solved this problem with a breakthrough.
• Breast Cancer. Every year, 50000 women are diagnosed with highly lethal HER-2 (+) breast cancer. Herceptin (trastuzumab) is the only biological therapy approved by FDA. Like all antibody therapies, their development, quality control, production, storage and dosage are expensive, and they cannot be taken orally. Moreover, their size limits their efficacy on solid tumors.
  Stable peptide therapy can greatly benefit patients with this disease by significantly reducing costs and providing potential oral routes of administration to increase the availability of treatment.

Key Benefits of PepDom™ Platform

Based on multi-disciplinary expertise and rich experience in peptidomimetic development, we continuously update our technology to meet the specific needs of customers in multiple fields.

• Efficient: High-throughput screening quickly discovers potential peptidomimetic molecules.
• Focus: Targeted development of peptidomimetic molecules for research purposes.
• Diversity: Non-limiting selection of peptidomimetics.
• Continuous: Continuously carry out technological innovation to meet customer needs.

If you want to collaborate with us or learn more about how we can support your project focusing on peptidomimetic development, please do not hesitate to contact us!

References

1. Zhang, G., Brown, J.S., Quartararo, A.J. et al. Rapid de novo discovery of peptidomimetic affinity reagents for human angiotensin converting enzyme 2. (2022). Communications Chemistry, 5: 8.
2. Sohrabi, C., Foster, A. & Tavassoli, A. (2020). Methods for generating and screening libraries of genetically encoded cyclic peptides in drug discovery. Nature Reviews Chemistry, 4: 90–101.