Scientific Contributions

Our peptide chemistry team is excited to announce a new publication in the journal “Circulation”, which highlights the outcome of a highly successful drug discovery collaboration with Merck & co.’s world-class drug discovery group (Kenilworth, New Jersey).

The publication describes the discovery of a novel series of Imidazopyrazine derivatives by IRBM’s drug discovery team. This novel series of SHP2 allosteric inhibitors, having an imidazopyrazine 6,5-fused heterocyclic system as central scaffold, showed an excellent potency in enzyme and cellular assays.

Innovative synthetic strategies giving access to a larger chemical space are of great importance to make the development of peptide therapeutics a faster and more efficient process. Katritzky salts, easily prepared from primary amines, offer peptide chemists a tool to achieve many chemical transformations in a straightforward manner.

We are delighted to publish our first paper of 2022 in the Journal of Pharmaceutical and Biomedical Analysis (Elsevier). Here we leveraged our peptide #ADME toolbox to gain a better understanding of the interplay between oligomerization, albumin binding and catabolism of lipidated peptides in the subcutaneous compartment, using #GLP-1 analogs as model peptides.

Following the first report in the Journal of Medicinal Chemistry in 2020, the IRBM peptide chemistry group is proud to announce a new publication on second generation, potent bi- and tricyclic PCSK9 inhibitor peptides in collaboration with the extraordinary drug discovery team at Merck & co.