Scientific Contributions Archivi

A Series of Novel, Highly Potent, and Orally Bioavailable Next-Generation Tricyclic Peptide PCSK9 Inhibitors

Scientific Contributions

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

In The News, Scientific Contributions

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 Publish In Science Translational Medicine On Using HTT-lowering Therapies To Slow Down Neurodegeneration In Huntington’s Disease

IRBM cited in UniQure publication on using HTT-lowering therapies to slow down neurodegeneration in Huntington’s Disease

Scientific Contributions

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

Scientific Contributions

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

Scientific Contributions

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

In The News, Scientific Contributions

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.

Comparison Of Different Protein Precipitation And Solid‐phase Extraction Protocols For The Study Of The Catabolism Of Peptide Drugs By LC‐HRMS

IRBM publishes in J. Peptide Science on methods to study catabolism, key to designing more stable peptides

Scientific Contributions

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.

IRBM & University of Rome publishes in PLOS on new chemotype with antiparasitic activity for treating sleeping sickness

Scientific Contributions

Trypanosoma brucei is a parasite responsible for human African trypanosomiasis, also known as sleeping sickness, a disease endemic in sub-Saharan Africa, with 70 million people at risk of infection. Current treatments are limited by their toxicity, administration in endemic countries and treatment resistance.

IRBM publishes on optimizing a new series of Trypanosoma brucei growth inhibitors, the parasite responsible of the sleeping sickness

Scientific Contributions

Human African trypanosomiasis (HAT), also known as sleeping sickness, is a parasitic disease that causes significant mortality in sub- Saharan Africa. A previous publication from IRBM laboratory reported the identification of 2-(1H-imidazo-2-yl)piperazines as a new series of potent T. brucei growth inhibitors.

IRBM & University of Rome publishes in Nature on crucial signaling pathway in muscle homeostasis and regeneration

Scientific Contributions

IRBM, working with the University of Rome’s Department of Biology, examined signaling pathways involved with the regulation of Fibro/Adipogenic Progenitors (FAPs). FAPs are muscle-interstitial progenitors mediating pro-myogenic signals that are critical for muscle homeostasis and regeneration.