Publications Archivi

Orally Bioavailable Macrocyclic Peptide That Inhibits Binding of PCSK9 to the Low Density Lipoprotein Receptor

Publications, Publications 2023, 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).

Katritzky Salts For The Synthesis Of Unnatural Amino Acids And Late-Stage Functionalization Of Peptides

IRBM’s drug discovery research is featured on the cover of this issue’s ACS Publications’ Medicinal Chemistry Letters

Publications, Publications 2023, Scientific Contributions

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.

IRBM review article on Katritzky salts (as intermediates for the synthesis of unnatural amino acids, late-stage functionalization of peptides, and macrocyclization) is featured on the cover of the European Journal of Organic Chemistry

Publications, Publications 2023, Scientific Contributions

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.

Discovery of MK-1462: GLP-1 and Glucagon Receptor Dual Agonist for the Treatment of Obesity and Diabetes

News, Publications, Publications 2022

The IRBM peptide chemistry team is proud to announce a new publication in ACS Medicinal Chemistry Letters in collaboration with the outstanding drug discovery team at Merck & Co. (Kenilworth, NJ).

IRBM publish malaria breakthrough research in Nature Communications Biology

News, Press Releases, Publications, Publications 2022

In a collaboration with Istituto Superiore di Sanità and CNR, IRBM has published research that identified new molecules which block the transmission of the malaria parasite from an infected person to the mosquito, the first step in developing new drugs to eliminate this major infectious disease.

SAR evolution towards potent C-terminal carboxamide peptide inhibitors of Zika virus NS2B-NS3 protease

Publications 2022, Scientific Contributions

Zika virus (ZIKV) is a member of the Flaviviridae family that can cause neurological disorders and congenital malformations.

Effect On Body Weight And Food Intake Of Short Term Administration Of DH-CNTF And PEG-DH-CNTF In DIO Mice

Efficacy of PEGylated ciliary neurotrophic factor superagonist variant in diet-induced obesity mice

Publications, Publications 2022

At IRBM, we are passionate about understanding the underlying biology of disease, to drive drugdiscovery. In a recent paper funded by our consortium partner CNCCS, we evaluated the efficacy of a PEGylated Ciliary Neurotrophic Factor (CNTF) super-agonist variant in diet-induced obese mice.

NRF2 activation by reversible KEAP1 binding induces the antioxidant response in primary neurons and astrocytes of a Huntington’s disease mouse model

Publications, Publications 2020

Oxidative stress has been associated with pathogenesis in several diseases including Huntington's disease (HD), a neurodegenerative disorder caused by a mutation in the huntingtin gene. Oxidative stress induced reactive oxygen species (ROS) are normally controlled at the cellular level by…

Analysis of mutant and total huntingtin expression in Huntington’s disease murine models

Publications, Publications 2020

Huntington's disease (HD) is a monogenetic neurodegenerative disorder that is caused by the expansion of a polyglutamine region within the huntingtin (HTT) protein, but there is still an incomplete understanding of the molecular mechanisms that drive pathology. Expression of the…

Cyclic Phosphopantothenic Acid Prodrugs for Treatment of Pantothenate Kinase-Associated Neurodegeneration

Publications, Publications 2020

Mutations in the human PANK2 gene are implicated in neurodegenerative diseases such as pantothenate kinase-associated neurodegeneration (PKAN) and result in low levels of coenzyme-A (CoA) in the CNS due to impaired production of phosphopantothenic acid (PPA) from vitamin B5. Restoration…

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