Publications 2022 Archivi

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.

Guiding chemically synthesized peptide drug lead optimization by de-risking mast cell degranulation related toxicities of a NaV1.7 peptide inhibitor

Publications, Publications 2022

Peptides can induce non IgE-mediated anaphylactoid reactions. These effects are triggered by the direct interaction of the peptide with mast cells that result in their degranulation and release of histamine and other inflammatory mediators.

Development of ProTx-II Analogues as Highly Selective Peptide Blockers of Nav1.7 for the Treatment of Pain

Publications, Publications 2022

Targeting ion channels involved in nociception is currently being investigated for the treatment of pain. Human genetic studies have demonstrated that patients with null mutations in the voltage-gated sodium channel Nav1.7 were resistant to pain suggesting that Nav1.7 could be a target for the development of novel analgesic. ProTx-II, a peptide toxin belonging to the inhibitory cystine knot (ICK) family, was shown to selectively block the Nav1.7 channel but lacked in vivo efficacy.

Oligomerization, albumin binding and catabolism of therapeutic peptides in the subcutaneous compartment: an investigation on lipidated GLP-1 analogs

Publications, Publications 2022, Scientific Contributions

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.

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