Lead Optimization Services

To use a lead peptide as a full-grown therapeutic drug, its potency must increase. Tap into the knowledge of Pepscan by using our design assistance. Our epitope mapping platform can identify small peptide binders designed or derived from whole protein sequences. We can also create constrained (e.g. CLIPS™) derivatives of lead sequences with significantly improved binding activity.

Alanine scanning libraries identify residues that play a key role in peptide activity. Alanine, the smallest chiral natural amino acid, is used to substitute residues at each position of the original peptide. The effect of alanine substitution on the overall peptide activity determines the importance of each individual residue.

Positional scanning is a key method for sequence optimization. By sequentially substituting selected amino acid residues for all other natural L-amino acids, residues crucial for activity can be identified. Substitutions displaying an improved activity can also be found.

Positional scanning library design usually starts by focusing on the naturally occurring L-amino acids. For tapping into the artificial amino acid space, non-natural amino acids can also be included. There are over 400 commercially available non-natural amino acids. Pepscan has 200 of these in stock, which can be readily implemented in your library design. We have another 300 non-natural amino acids in our database, which can be included on request.