Therapeutic peptide discovery
The strong and unique combination of peptide arrays and CLIPS technology creates an excellent technology platform for therapeutic peptide drug discovery, in particular peptide lead identification and lead optimization. The CLIPS peptide arrays are well-suited for the mapping of any type of protein-protein interactions (PPIs) e.g. between peptide ligands and proteins. These interactions can be detected with a high degree of specificity using the high throughput array screening format. The technology is most easily applied to improve the affinity/activity of an existing lead peptide, but also has great value for lead finding purposes.
The lead optimization involves chemical modifications of a therapeutic peptide in order to improve potency, selectivity or pharmacokinetic parameters. Pepscan has validated from several studies that by applying the CLIPS technology to selected peptides their affinity is increased and hence bioactivity is improved. As a result, the use and insertion of CLIPS may lead to the generation of New Chemical Entities (NCEs) which also opens new options for IP.
Apart from activity improvement, the use of CLIPS templates has also shown great value for improving the proteolytic stability of a peptide. Since the thioether bonds between the CLIPS template and the peptide are non-natural, they provide stability towards degradative enzymes. Morever, CLIPSed peptides often have a better defined 3D-structure which also protects against proteolytic degradation.