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In pharmaceutical chemistry and drug discovery, the technology of transforming peptides into drug precursors is still a dynamic and fertile field. Peptidomimetic can compensate for peptide restriction by showing higher metabolic stability, good bioavailability and enhanced receptor affinity and selectivity. CD BioSciences can use its peptide discovery platform based on mRNA display technology to provide customers with a variety of peptide development services.
Due to the progress in structure optimization, formulation and production, more and more peptides have entered clinical trials and been approved as drugs. However, these molecules still have some shortcomings, such as the limited stability of protein hydrolysis, resulting in a short half-life in the gastrointestinal tract and serum; Relatively high molecular weight and lack of specific transport system lead to poor absorption and transport performance; The N-Ca and Ca-CO rotary bonds on amino acids have inherent flexibility, resulting in poor selectivity and unexpected side effects. Peptidomimetic have been developed with metabolic stability, good bioavailability, high receptor affinity and selectivity by introducing modifications that can solve the inherent shortcomings of peptides while maintaining the structural characteristics responsible for biological activity. Their emergence has made up for the inherent defects of existing peptides and become a new generation of peptide therapy for a variety of diseases and mechanism research.
Fig. 1 B-D-glucose based somatostatin-14 peptidomimetic.
(Lenci, et al., 2020)
There are three main methods of peptidomimetic design and synthesis. The selection of design strategy depends on the understanding of target protein in terms of structure, sequence, function and protein-binding site characteristics. When the sequence of bioactive peptide is known, it can be developed by local modification; Or use 3D pharmacodynamics model to carry out reasonable design. When the structure or pharmacodynamic model of bioactive peptides is unknown, the only possible method is to randomly screen large peptide libraries. The mRNA display can construct a 1012-1014 capacity peptide library by random sequence design, and can introduce unnatural amino acids to modify the peptide chain. Because it does not undergo cell transformation, it can generally obtain high affinity target peptidomimetic molecules through four rounds of display cycle screening
mRNA display technology covalently connects genotype and phenotype through purinomycin, and screen peptides and proteins in vitro, which shows better adaptability and stability to experimental conditions. CD BioSciences has established a peptide discovery platform based on mRNA display technology to provide customers around the world with various types of peptidomimetic development services to meet different research needs. The direction we can develop:
Different Targets |
Different Diseases |
Different Functions |
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Our peptidomimetic development service is based on high-throughput screening by constructing a peptide library when the lead peptide sequence information is unknown. Therefore, you only need to provide us with specific project purpose information, and our experts can carry out scheme design based on this. In addition, we also provide the development services of restrictive peptides, including the development of Macrocyclic Peptide Development and Stapled Peptide Development.
1. Transcription and Purinomycin Ligation
2. Translation and Modification
3. Reverse Transcription
4. Affinity Screening of Immobilized Target
5. Recovery by PCR
6. Cyclic Display to Obtain Target Peptidomimetic
CD BioSciences has many years of project development experience in peptide discovery. Based on the mRNA display technology platform, it can provide customers with multiple peptidomimetic development services. If you are interested in our services, please contact us for more details.
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