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

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.

Statistics

0100020002017
Citations per Year

238 Citations

Semantic Scholar estimates that this publication has 238 citations based on the available data.

See our FAQ for additional information.

Cite this paper

@article{Stucchi2016DisruptingTP, title={Disrupting the PCSK9/LDLR protein-protein interaction by an imidazole-based minimalist peptidomimetic.}, author={Mattia Stucchi and Giovanni Grazioso and Carmen Lammi and Silvia Manara and Chiara Zanoni and Anna Arnoldi and Giordano Lesma and Alessandra Silvani}, journal={Organic & biomolecular chemistry}, year={2016}, volume={14 41}, pages={9736-9740} }