Second generation mimics of ganglioside GM1 as artificial receptors for cholera toxin: Replacement of the sialic acid moiety

被引:28
作者
Bernardi, A
Carrettoni, L
Ciponte, AG
Monti, D
Sonnino, S
机构
[1] Univ Milan, Dipartimento Chim Organ & Ind, I-20133 Milan, Italy
[2] CNR, Ctr Studio Sostanze Organ Nat, I-20133 Milan, Italy
[3] Univ Milan, LITA, Dipartimento Chim & Biochim Med, Segrate, MI, Italy
关键词
D O I
10.1016/S0960-894X(00)00428-5
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
In a program directed towards the design and synthesis of mimics of ganglioside GM1, the NeuAc recognition domain was replaced by simple hydroxy acids, and the affinity of the new ligands to the cholera toxin was determined by fluorescence spectroscopy. The (R)-lactic acid derivative 4 was found to display the highest affinity of the series (K-D = 190 mu M). (C) 2000 Elsevier Science Ltd. All rights reserved.
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页码:2197 / 2200
页数:4
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