Peptide Lead Optimization

Do you need to improve the affinity of your lead peptide? Does your lead peptide not yet display the high activity for the target needed for an active drug that also works in vivo? Pepscan’s Lead Optimization brings your candidate peptide to the next level. Our highly skilled team is well-equipped with many years of experience in peptide lead optimization.

What is Peptide Lead Optimization?

Lead optimization is a critical step in the design of novel peptide-based drugs. Most peptide leads display interesting properties for therapeutic drugs, but the binding is suboptimal. Typical affinities to the target protein are usually in the (sub)micromolar range, or the stability to proteolytic degradation is insufficient. This is where Pepscan’s Lead Optimization team comes in.

Peptide Leads Can Be Optimized in Three Ways

  1. Through amino acid replacement analysis
  2. By constraining peptides using CLIPS™ technology
  3. By improving the peptide length or size

By combining these modifications in iterative screening rounds, Pepscan can improve the affinity of peptide-based lead drug candidates up to 1,000 times.

Read more on the achievements of Pepscan

Pepscan’s Lead Optimization Services

  1. Support in designing the most efficient and economic library to help you compute lists of peptide library sequences
  2. Unique libraries of 3D-constrained (CLIPS™) peptides if the 3D conformation of your peptide is crucial
  3. A wide range of library design options, each tailored to your specific research questions
  4. Peptide libraries produced with different types of non-natural amino acid variants, such as 1- or 2-naphthylalanine, tert-butylalanine, nor-isoleucine, nor-leucine, nor-valine, etc., or backbone N-methylations, or typical post-translational modifications, such as serine/threonine/tyrosine phosphorylation or arginine/lysine methylations

Read more about our Lead Optimization services

Why Choose Lead Optimization at Pepscan?

  • Detailed insights into the critical amino acids of a lead peptide
  • Improved binding affinity by introducing a large variety of non-natural amino acids
  • Additional insights through mutational analysis and alanine scanning (AlaScan)
  • Development of an enhanced molecule by constraining it (e.g. using CLIPS™) for better pharmacokinetic properties, resulting in improved specificity, complex stability, and decreased elimination/clearance, which directly affects the potency of a lead drug candidate
  • Possibility to include various in-house functional assays to determine proteolytic and/or enzymatic stability profiles of a lead peptide candidate

ADMET & DMPK Services

For peptide drugs, formation of toxic or harmful metabolites is of minor importance. However, proteolytic degradation of the peptide (by means of exo- or endoproteases) is often observed since truncated sequences can be formed. For this sort of MetID, Pepscan offers a limited service addressing the enzymatic degradation of peptides, for instance in blood serum or blood plasma. Please contact us to learn more about this service. Note that Pepscan does not offer ADMET & DMPK services beyond this.

Our work

Want to read more on Peptide Lead Optimization? Click below to read more about our work.

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