Lead Optimization resources

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.

Broaden the Horizon: Find New Chemical Entities by Introducing BiBridged™ Cyclization Topologies

The new BiBridged™ technology displays huge potential for peptide lead discovery and optimization, opening the possibility to identify small-sized and highly stable peptide ligands. Developing these small and compact ligands is challenging because they have fewer amino acids interacting with the target than the natural ligands. This handicap can be overcome by generating a molecular shape perfectly complementary to the target binding site, and subsequently “freezing” this shape in 3D. This creates a small but potent and highly selective binder, superior even to monoclonal antibodies. In this blog, we introduce the BiBridged™ peptide topology and illustrate its possibilities.

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Bring Your Candidate Peptide to the Next Level with Lead Optimization

Lead optimization is a critical step in the design of novel peptide-based drugs. Peptide microarray screening is frequently used in the optimization of lead peptides by replacing every amino acid in the sequence. The goal is to increase peptide drug potency and improve pharmacokinetic properties. In this blog, we explain how lead optimization by microarray screening works, as described in four different case studies. In all cases, full replacement analysis improved the affinity and pharmacokinetic properties of the lead peptide.

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Pepscan Brochure Peptide Lead Optimization

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 helps you bring your candidate peptide to the next level. Our highly skilled project team is well-equipped with many years of experience in peptide lead optimization. Open the brochure, and read about what Peptide Lead Optimization is, three ways to optimize Peptide Leads, what Pepscan offers, and why to choose Lead Optimization at Pepscan.

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Pepscan Whitepaper Lead Identification and optimalization

How to specifically kill invading microbes using chemicals, like a bullet fired from a gun? This question forms the basis of the “magic bullet” concept of 20th century Nobel Prize laureate Paul Ehrlich. His work helped lay the foundation of immunology, and Ehrlich’s vision has been tackled by many drug developers since. In this respect, multicyclic peptides are getting close to perfect. They are increasingly being utilized as a homing device – to bring cytotoxic killing agents into cancers with unprecedented effectivity and success, creating little to no side effects. In this whitepaper, we illustrate how the affinity and selectivity of bicyclic RGD peptides were optimized from scratch in a stepwise manner, finally reaching an extraordinary level when compared to the field’s standard compounds.

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