基于对称五价神经节苷脂 GM1os-sym-corannulenes 的纳摩尔霍乱毒素抑制剂。
Nanomolar cholera toxin inhibitors based on symmetrical pentavalent ganglioside GM1os-sym-corannulenes.
机构信息
Institute of Organic Chemistry, University of Zurich, Winterthurerstrasse 190, 8057 Zurich, Switzerland.
Laboratory of Organic Chemistry, Wageningen University, Dreijenplein 8, 6703 HB, Wageningen, The Netherlands.
出版信息
Org Biomol Chem. 2013 Jul 14;11(26):4333-4339. doi: 10.1039/c3ob40438b. Epub 2013 Jun 4.
Eight symmetric and pentavalent corannulene derivatives were functionalized with galactose and the ganglioside GM1-oligosaccharide (GM1os) via copper-catalyzed alkyne-azide cycloaddition (CuAAC) reactions. The compounds were evaluated for their ability to inhibit the binding of the pentavalent cholera toxin to its natural ligand, ganglioside GM1. In this assay, all ganglioside GM1os-sym-corannulenes proved to be highly potent nanomolar inhibitors of cholera toxin.
通过铜催化的叠氮-炔环加成（CuAAC）反应，将 8 个对称的五价 corannulene 衍生物与半乳糖和神经节苷脂 GM1-寡糖（GM1os）官能化。评估了这些化合物抑制五价霍乱毒素与其天然配体神经节苷脂 GM1 结合的能力。在该测定中，所有神经节苷脂 GM1os-对称 corannulenes 均被证明是霍乱毒素的高活性纳摩尔抑制剂。
Zotero 插件