Issue 41, 2016
From the journal:

Organic & Biomolecular Chemistry

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

Mattia Stucchi,*ab   Giovanni Grazioso, ORCID logo *c   Carmen Lammi,*c   Silvia Manara,c   Chiara Zanoni,c   Anna Arnoldi,c   Giordano Lesmaa  and  Alessandra Silvani ORCID logo a  

* Corresponding authors

a Dipartimento di Chimica, Università degli Studi di Milano, Via Golgi 19, 20133 Milano, Italy
E-mail: mattia.stucchi@unimi.it

b Dipartimento di Scienze della Vita, Università di Modena e Reg-gio Emilia, via G. Campi 103, 41125 Modena, Italy

c Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, Via L. Mangiagalli 25, 20133 Milano, Italy
E-mail: giovanni.grazioso@unimi.it, carmen.lammi@unimi.it

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.

Graphical abstract: Disrupting the PCSK9/LDLR protein–protein interaction by an imidazole-based minimalist peptidomimetic

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Article information

DOI
https://doi.org/10.1039/C6OB01642A
Article type
Communication
Submitted
30 Jul 2016
Accepted
27 Sep 2016
First published
27 Sep 2016
This article is Open Access
Creative Commons BY-NC license

Org. Biomol. Chem., 2016,14, 9736-9740

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

M. Stucchi, G. Grazioso, C. Lammi, S. Manara, C. Zanoni, A. Arnoldi, G. Lesma and A. Silvani, Org. Biomol. Chem., 2016, 14, 9736 DOI: 10.1039/C6OB01642A

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