2. Academic Validation
  3. Disrupting the PCSK9/LDLR protein-protein interaction by an imidazole-based minimalist peptidomimetic

Disrupting the PCSK9/LDLR protein-protein interaction by an imidazole-based minimalist peptidomimetic

  • Org Biomol Chem. 2016 Oct 18;14(41):9736-9740. doi: 10.1039/c6ob01642a.
Mattia Stucchi 1,  Giovanni Grazioso 2,  Carmen Lammi 2,  Silvia Manara 2,  Chiara Zanoni 2,  Anna Arnoldi 2,  Giordano Lesma 3,  Alessandra Silvani 3
Affiliations

Affiliations

  • 1 Dipartimento 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.
  • 2 Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, Via L. Mangiagalli 25, 20133 Milano, Italy. giovanni.grazioso@unimi.it carmen.lammi@unimi.it.
  • 3 Dipartimento di Chimica, Università degli Studi di Milano, Via Golgi 19, 20133 Milano, Italy. mattia.stucchi@unimi.it.
PMID: 27722650 DOI: 10.1039/c6ob01642a
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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