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.
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, A. Silvani. - In: ORGANIC & BIOMOLECULAR CHEMISTRY. - ISSN 1477-0539. - 14:41(2016 Oct 06), pp. 9736-9740.
Titolo: | Disrupting the PCSK9/LDLR protein-protein interaction by an imidazole-based minimalist peptidomimetic |
Autori: | LESMA, GIORDANO (Penultimo) SILVANI, ALESSANDRA (Ultimo) |
Settore Scientifico Disciplinare: | Settore CHIM/08 - Chimica Farmaceutica Settore CHIM/06 - Chimica Organica |
Data di pubblicazione: | 6-ott-2016 |
Rivista: | |
Tipologia: | Article (author) |
Digital Object Identifier (DOI): | http://dx.doi.org/10.1039/c6ob01642a |
Appare nelle tipologie: | 01 - Articolo su periodico |
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