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Updated: Mar 13, 2026

A High-Throughput Luciferase Assay to Evaluate Proteolysis of the Single-Turnover Protease PCSK9
Published on: August 28, 2018
Disrupting the PCSK9/LDLR protein-protein interaction by an imidazole-based minimalist peptidomimetic
Mattia Stucchi1, Giovanni Grazioso2, Carmen Lammi2
1Dipartimento di Chimica, Università degli Studi di Milano, Via Golgi 19, 20133 Milano, Italy. mattia.stucchi@unimi.it and Dipartimento di Scienze della Vita, Università di Modena e Reg-gio Emilia, via G. Campi 103, 41125 Modena, Italy.
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.
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