通过基于咪唑的简约拟肽破坏前蛋白转化酶枯草溶菌素9（PCSK9）/低密度脂蛋白受体（LDLR）蛋白-蛋白相互作用。
Disrupting the PCSK9/LDLR protein-protein interaction by an imidazole-based minimalist peptidomimetic.
作者信息
Stucchi Mattia, Grazioso Giovanni, Lammi Carmen, Manara Silvia, Zanoni Chiara, Arnoldi Anna, Lesma Giordano, Silvani Alessandra
机构信息
Dipartimento di Chimica, Università degli Studi di Milano, Via Golgi 19, 20133 Milano, Italy.
Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, Via L. Mangiagalli 25, 20133 Milano, Italy.
出版信息
Org Biomol Chem. 2016 Oct 18;14(41):9736-9740. doi: 10.1039/c6ob01642a.
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.
在此，我们报道了一种新型咪唑基化合物的多组分合成，该化合物能够有效地作为一种极简主义的β-链模拟物发挥作用。生物学评估证明了其破坏低密度脂蛋白受体（LDLR）-前蛋白转化酶枯草溶菌素9（PCSK9）蛋白-蛋白相互作用的能力，表明它是第一种发挥PCSK9介导的降胆固醇作用的小分子。
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