Unit Head: Elisabetta Bianchi

As a former Merck Research Laboratories “Peptide Center of Excellence”, the peptide chemistry group at IRBM Science Park has a world-class expertise in the development of peptide therapeutics with a track record in the clinic.

IRBMThe team has extensive experience in different therapeutic areas, and our focus is on target identification/validation and lead optimization.

The hit-to-lead process proceeds from peptide engineering and design, through multi-parametric optimization for activity, efficacy and selectivity. The discovery phase takes advantage of a large collection of non-natural amino acids (>500, commercial or ad hoc synthesized) and chemical constraints to stabilize the active conformation.

Multiple approaches to lead optimization include: peptidomimetic chemistry, backbone modifications, macrocyclic stabilization and orthogonal conjugation.

Pharmacokinetics profiles are optimized by modifying peptide structures to overcome rapid metabolism and disposition due to enzymatic degradation and renal clearance. Finally, potential anaphylactic effects caused by mast cell activation and histamine release can be assessed in vitro, ensuring a cost-effective way of identifying dangerous responses prior to entering in vivo trials.

An integrated platform of different areas of expertise expands our peptide discovery efforts with additional tools, including the use of our phage display libraries, structural studies through NMR and the bio.analysis of peptides for in vivo studies supported by the Preclinical& Analytical Group with state-of-the-art mass spectrometry instrumentations.

The peptide chemistry team has also a strong background in synthetic capabilities providing peptide tools for basic research, including targets comprising long and difficult peptide sequences.

Unit Capabilities

  • Peptide design and engineering;
  • Peptidomimetic chemistry;
  • Backbone modifications;
  • Macrocyclic stabilization;
  • Orthogonal conjugation;
  • Pharmacokinetics optimization;
  • Anaphylactic reaction risk mitigation;
  • Peptide synthesis through microwave-assisted solid phase assemply;
  • Assembly of peptide fragments through native chemical ligation;
  • Semi-synthetic approaches to post-translational modifications.