Disrupting the PCSK9/LDLR protein–protein interaction by an imidazole-based minimalist peptidomimetic†
Abstract
Herein we report on the multicomponent synthesis of a novel imidazole-based compound, able to act efficiently as a minimalist β-strand mimic. Biological evaluation proved its ability to impair the LDLR–PCSK9 protein–protein interaction, disclosing it as the first small molecule exerting a PCSK9-mediated hypocholesterolemic effect.