Nanomolar cholera toxin inhibitors based on symmetrical pentavalent ganglioside GM1os-sym-corannulenes
Nanomolar cholera toxin inhibitors based on symmetrical pentavalent ganglioside GM1os-sym-corannulenes
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DOI：
10.1039/c3ob40438b
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发表时间：
2013-01-01
影响因子：
3.2
通讯作者：
Siegel, Jay S.
中科院分区：
文献类型：
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作者：
Mattarella, Martin;Garcia-Hartjes, Jaime;Siegel, Jay S.
通过铜催化的炔-叠氮环加成（CuAAC）反应，将八种对称的五价corannulene衍生物与半乳糖和神经节苷脂GM 1-寡糖（GM 1 os）进行功能化.评价化合物抑制五价霍乱毒素与其天然配体神经节苷脂GM 1结合的能力。在该测定中，所有神经节苷脂GM 1 os-sym-corannulenes被证明是霍乱毒素的高效纳摩尔抑制剂。
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.