Published in
Royal Society of Chemistry, Organic and Biomolecular Chemistry, 41(14), p. 9736-9740
DOI: 10.1039/c6ob01642a
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Disrupting the PCSK9/LDLR protein-protein interaction by an imidazole-based minimalist peptidomimetic
Journal article published in 2016 by
Mattia Stucchi,
Giovanni Grazioso 
,
Carmen Lammi,
Silvia Manara,
Chiara Zanoni,
Anna Arnoldi,
Giordano Lesma,
Alessandra Silvani
,
Carmen Lammi,
Silvia Manara,
Chiara Zanoni,
Anna Arnoldi,
Giordano Lesma,
Alessandra Silvani
This paper is made freely available by the publisher.
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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.