Strong inhibition of cholera toxin by multivalent GM1 derivatives

Strong inhibition of cholera toxin by multivalent GM1 derivatives
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DOI:
10.1002/cbic.200700266
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发表时间:
2007-09-03
期刊:
影响因子:
3.2
通讯作者:
Pieters, Roland J.
Pieters, Roland J.
中科院分区:
生物学3区
文献类型:
--
作者:
Pukin, Aliaksei V.;Branderhorst, Hilbert M.;Pieters, Roland J.

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(提出化学方程式)粘手指。霍乱毒素 (CT) 的最佳配体 GM1-寡糖 (GM1os) 通过使用高效的“点击”化学偶联与包含长间隔臂的树突结构连接。在抑制研究中观察到非常大的多价效应;最好的结构是前所未有的比单价 GM1os 衍生物强 380 000 倍的毒素配体
(Chemical Equation Presented) Sticky fingers. The optimal ligand for the cholera toxin (CT), GM1-oligosaccharide (GM1os), was linked to dendritic structures that contained long spacer arms by using highly efficient "click" chemistry coupling. In the inhibition studies very large multivalency effects were observed; the best structure was an unprecedented 380 000-fold more potent ligand for the toxin than a monovalent GM1os derivative