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 contribution to Medicinal Chemistry Letters by the American Chemical Society
We are pleased to have contributed multiple articles to the Italian special edition of ACS Medicinal Chemistry Letters, highlighting the world-class drug discovery research taking place at IRBM.
One of our studies featured in this publication, deals with an exploratory program aimed at identifying selective inhibitors of isoform-2 acid-sensing ion channels (ASIC-2). ASIC is a family of proton-activated ion channels widely expressed both in central and peripheral nervous system, as well as in cancer cells, and may represent a relevant target for drug discovery. Diminazene, a known ASIC inhibitor endowed with poor target specificity and negligible blood-brain barrier penetration, was used as a chemical starting point for optimization. Compound 2u was identified as the first selective and brain penetrant ASIC-2 inhibitor, as a useful tool to validate the role of ASIC-2 isoform in different type of neurodegenerative pathologies.
Read more here.
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