Synthesis of perylene bisimide-centered glycodendrimer and its interactions with concanavalin A.

Synthesis of perylene bisimide-centered glycodendrimer and its interactions with concanavalin A.
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DOI:
10.1016/j.bmcl.2012.11.049
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发表时间:
2013-01
影响因子:
2.7
通讯作者:
Ke-Rang Wang;Yue-qing Wang;Jie Li;Hong-Wei An;Liping Zhang;Jinchao Zhang;Xiao-liu Li
Ke-Rang Wang;Yue-qing Wang;Jie Li;Hong-Wei An;Liping Zhang;Jinchao Zhang;Xiao-liu Li
中科院分区:
医学4区
文献类型:
--
作者:
Ke-Rang Wang;Yue-qing Wang;Jie Li;Hong-Wei An;Liping Zhang;Jinchao Zhang;Xiao-liu Li

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合成了一种基于18个α-d-甘露糖修饰的苝酰亚胺衍生物PBI-18-Man,并通过圆二色光谱和浊度法研究了其与刀豆蛋白A(ConA)的选择性结合作用,其结合常数为1.3× 108 M −1(单体甘露糖为7.2× 106 M − 1,化合价校正),亲和力比单价甘露糖配体高3个数量级。用ELLA法测定了该化合物对Con A的抑制活性,其抑制活性是参比化合物(α-MMP)的2倍。
A novel glycodendrimer based on 18 peripheral α-d-mannoses functionalized perylene bisimide derivative PBI-18-Man was synthesized and its selectively binding interactions for Con A were investigated by CD spectra and turbidity assay, which exhibited strong binding affinity for Con A with the binding constant of 1.3×108M−1(7.2×106M−1for monomeric mannose, valency corrected), 3 orders of magnitude higher affinity than the monovalent mannose ligand. Furthermore, the inhibitory activity for Con A was studied by ELLA experiment, showed 2 times inhibitor activity than the reference compound (α-MMP).