SAR evolution towards potent C-terminal carboxamide peptide inhibitors of Zika virus NS2B-NS3 protease
Zika virus (ZIKV) is a member of the Flaviviridae family that can cause neurological disorders and congenital malformations.
IRBM GEN Cell Imaging
This month Genetic Engineering & Biotechnology News features IRBM in an article about ‘Image-based high-content screening and predictive cell-based assays for drug discovery and development.’
Oligomerization, albumin binding and catabolism of therapeutic peptides in the subcutaneous compartment: an investigation on lipidated GLP-1 analogs
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.
A Series of Novel, Highly Potent, and Orally Bioavailable Next-Generation Tricyclic Peptide PCSK9 Inhibitors
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.
Discovery and characterization of novel peptide inhibitors of the NRF2/MAFG/DNA ternary complex for the treatment of cancer
Our Peptide Chemistry team, in collaboration with scientists at Merck and Co., reported on the design, synthesis and characterization of potent and stable peptides able to inhibit the binding of NRF2-MAFG heterodimeric transcription factor to Antioxidant Response Element (ARE) DNA sequence.
IRBM cited in UniQure publication on using HTT-lowering therapies to slow down neurodegeneration in Huntington’s Disease
UniQure has just published a study in Science Translational Medicine using a Huntingtin (HTT)-lowering therapy. IRBM is delighted to have been able to contribute to this pivotal work and to be cited on the publication. Huntingtin is the gene that…
Identification of Potent and Long-Acting Single-Chain Peptide Mimetics of Human Relaxin-2 for Cardiovascular Diseases
Our integrated drug discovery efforts on the Relaxin-2 peptide hormone, in collaboration with our collaborators at global life sciences company Sanofi, has produced a paper just published in the Journal of Medicinal Chemistry. The natural peptide hormone human relaxin-2 has…
Series of Novel and Highly Potent Cyclic Peptide PCSK9 Inhibitors Derived from an mRNA Display Screen and Optimized via Structure-Based Design
In the last few years macrocyclic peptides have emerged as a better class of lead candidates for inhibition of protein-protein interactions with respect to conventional small molecules. The IRBM peptide chemistry team collaborated with the teams at Merck & co. and RaPharma to develop potent macrocyclic peptide inhibitors of PCSK9 a key regulator of plasma LDL-cholesterol.
IRBM & collaborators publish on techniques for characterizing peptides in Type 2 diabetes and a peptide drug discovery program for Huntington’s disease
Nowadays, there is a strong drive to explore new areas of chemical space in search of innovative ways to bind and modulate challenging biological targets. At IRBM our peptide chemistry team has extensive expertise in peptide and macrocyclic drug discovery in various therapeutic areas.
IRBM publishes in J. Peptide Science on methods to study catabolism, key to designing more stable peptides
IRBM used liquid chromatography-high resolution mass spectrometry to explore different methods for the study of catabolism (breakdown) which is a key driver in the design of more stable peptides.