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At IRBM, we harness our world-class expertise in the development of safe and effective peptide therapeutics. Our team has extensive knowledge in peptide and macrocyclic drugs. This expertise has been built over decades, during which time our team has made significant contributions to the field, in particular as the “Peptide Center of Excellence” for Merck Research Laboratories (MRL). Since becoming independent in 2010, our scientists contributed to many published scientific studies and have been listed as inventors in more than 25 patent applications filed with our collaborators.

We use our extensive knowledge in the design of peptides and macrocycles to advance drug discovery programs. We have proven success in developing candidates, including macrocycles incorporating multiple constraints and peptide conjugates. Main areas of applications are peptide hormone optimization, macrocycles targeting protein/protein interactions and peptide ligands for theranostic applications.

THE PEPTIDE DISCOVERY PROCESS

Peptide leads targeting receptors/proteins of interest, including on cells, can be identified by screening our peptide libraries using IRBM’s phage display technology or by mRNA display through our collaborators. Our workflow for peptide drug development exploits extensive design and engineering to optimize multiple parameters. We employ integrated approaches such as advanced synthetic strategies, high throughput screening, ADME studies, NMR structural studies to optimize activity, efficacy and selectivity generating novel intellectual property.

We improve pharmacokinetic profiles to overcome rapid metabolism and disposition due to enzymatic degradation and renal filtration and use high resolution mass spectrometry to identify peptide metabolites from both in vitro and in vivo samples. In addition, we screen for potential pseudo-allergic reactions due to mast cell activation and histamine release to ensure only promising candidates are pursued.

Chemical strategies

Using advanced synthetic strategies, our team designs and synthesizes complex peptides, delivering tools such as long and difficult peptide sequences, labelled peptides, and small proteins with synthetic or post-translational modifications. Our strategies include:

  • Microwave-assisted solid phase chemistry
  • Pseudo-proline chemistry
  • Multi-analogue synthesis
  • Combined approaches between solution and solid-phase chemistry
  • Wide in-house collection of non-natural amino acids
  • Ad hoc synthesis of novel amino acids and building blocks
  • Backbone modification and cyclization chemistries
  • Chemo-selective conjugation chemistry
  • Native chemical ligation
ADDITIONAL WAYS WE CAN SUPPORT YOUR PEPTIDE DRUG DISCOVERY:
Peptide Chemistry Facility
Relevant Publications

PEPTIDE
DRUGS

MACROCYCLIC
PEPTIDES

PEPTIDE CONJUGATION
CHEMISTRY

COMPLEX
PEPTIDES & PROTEINS

PEPTIDE PAGE
DISPLAY

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