Amylovis-201 is a new dual-target ligand, acting as an anti-amyloidogenic compound and a potent agonist of the σ ₁ chaperone protein.

ABSTRACT: The aggregation of Amyloid-β (Aβ) peptides is associated with neurodegeneration in Alzheimer's disease (AD). We previously identified novel naphtalene derivatives, including the lead compound Amylovis-201, able to form thermodynamically stable complexes with Aβ species, peptides and fibrils. As the drug showed a chemical scaffold coherent for an effective interaction with the σ ₁ receptor chaperone and as σ ₁ agonists are currently developed as potent neuroprotectants in AD, we investigated the pharmacological action of Amylovis-201 on the σ ₁ receptor. We report that Amylovis-201 is a potent σ ₁ agonist by several in silico, in vitro and in vivo assays and that its anti-amnesi

SUBMITTER: Garcia-Pupo L 

PROVIDER: S-EPMC11544189 | biostudies-literature | 2024 Oct

REPOSITORIES: biostudies-literature