Bioactive Peptide Screening Technology
The pharmaceutical industry is currently facing tremendous pressure to accelerate and reduce the cost of novel drug development. This is an unfortunate challenge, primarily due to the limited selection of suitable toolsets at present to rapidly delineate and prioritize potential drug targets, and to screen for new high-specificity and low-toxicity drugs en masse. Peptide libraries can be used as tools for drug discovery by addressing the major causes of drug failure and by offering a cost-effective process from target validation to hit identification.
Recent innovations in the design of highly effective peptide pharmaceuticals, high throughput (HT) synthesis of extra long oligonucleotide on microarray surfaces, and HT sequencing provide us with a unique opportunity to develop the next generation of peptide libraries for HT screening of biologically active peptides in disease-relevant cell models (Figure 1).
Fig. 1. Summary of HT screening for bioactive peptides, from peptide library construction to hit validation.
To date, almost all cell-based primary screens employ strategies based on individual testing of hundreds of thousands of small molecules in arrayed formats. Cellecta's peptide libraries, based on viral delivery and expression, have the great advantage of simultaneously testing a complex pool of thousands of peptide compounds for biological activity; this process is very challenging with small molecules due to their toxicity in mixtures. In addition, peptide libraries, due to the variety of functional groups organized in constrained stable folds, may be able to replace small molecules in primary screens for a variety of extracellular drug targets.
Peptide leads have traditionally been derived from three sources: natural protein/peptides, synthetic peptide libraries, and recombinant libraries. As potential therapeutics, peptides offer several advantages over small molecules (increased specificity and affinity, low toxicity) and antibodies (small size).
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