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.
Disrupting the PCSK9/LDLR protein-protein interaction by an imidazole-based minimalist peptidomimetic
M. Stucchi
;G. Grazioso
;C. Lammi
;C. Zanoni;A. Arnoldi;G. LesmaPenultimo
;A. SilvaniUltimo
2016
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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