Peptide Screening and Optimization

1.What are the applications of small bioactive peptides in drug research?

Small bioactive peptides can be used in the development of vaccines, diagnostic reagents, drugs, and drug lead compounds, and have become a prominent trend in pharmaceutical research.

2.What is phage display peptide library screening?

Phage display peptide libraries are a mature method in which desired clones are obtained through three rounds of screening. DNA sequencing is then used to deduce the peptide sequences, which are subsequently synthesized to verify biological activity.

• Advantages: Mature methodology; widely applied.
• Disadvantages: Library diversity can be affected; the affinity of selected small peptides may be relatively low.

3.What are the characteristics of random synthetic peptide libraries?

They can be synthesized according to experimental needs, with a short production cycle and large library capacity (e.g., a 10-mer peptide library can reach 10¹² sequences).

Synthesis methods:

• Split-and-mix method: Each resin bead contains only one peptide, ensuring uniform sequence representation.
• Amino acid pre-mix method: Sequence representation can vary significantly, increasing the risk of screening failure.

4.What are the characteristics of antisense peptide library screening?

• Designed based on key amino acid sequences of the target protein, leading to a higher success rate.
• Smaller library size (e.g., a 10-mer antisense peptide library contains ~10³ sequences), making screening and structural verification easier.
• Key regions can be compared using software such as Clustal X, or screened via theoretical models like Meker-Idlis or simulations in Discovery Studio.

5.How can peptide activity be further optimized?

• Single-point scanning matrix: Systematically substitutes specific amino acids in the peptide; suitable for small-scale screening.
• Multi-site scanning random peptide library: Simultaneously substitutes multiple residues, greatly increasing library size and screening throughput (e.g., triple-site scanning can reach ~8000 variants).

• Proprietary combinatorial chemistry strategies (e.g., Peptidego™): Significantly reduce synthesis and screening workload; for example, triple-site scanning can be reduced to ~800 variants while supporting more site scans, enhancing screening efficiency.

Aladdin: https://www.aladdinsci.com/