Liposome-like fucopeptides as sialyl Lewis X mimetics

被引:26
|
作者
Lin, CC [1 ]
Kimura, T [1 ]
Wu, SH [1 ]
WeitzSchmidt, G [1 ]
Wong, CH [1 ]
机构
[1] Scripps Res Inst, DEPT CHEM, LA JOLLA, CA 92037 USA
关键词
D O I
10.1016/S0960-894X(96)00509-4
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Several fucodipeptides and their liposome-like derivatives were prepared and tested as inhibitors of sialyl Lewis X binding to E-selectin. It has been found that trans-hydroxyproline (D or L) can be used to mimic the galactose residue of sialyl Lewis X, and the mimetic containing 3,4-dihydroxy-D-proline is the most active with IC50 value (50 mu M) 10-fold greater than sialyl Lewis X. Derivatization of a hydroxythreonine-containing fucodipeptides into a covalent liposome-like derivative, however, provides a mimetic with only IC50 similar to 30 mu M. Copyright (C) 1996 Elsevier Science Ltd
引用
收藏
页码:2755 / 2760
页数:6
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