Probing the interactions of phosphosulfomannans with angiogenic growth factors by surface plasmon resonance

被引：76

作者：

Cochran, S

Li, CP

Fairweather, JK

Kett, WC

Coombe, DR

Ferro, V

机构：

[1] Progen Ind Ltd, Drug Design Grp, Brisbane, Qld 4077, Australia

[2] Curtin Univ Technol, Sch Biomed Sci, Div Hlth Sci, Perth, WA 6001, Australia

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 46卷 / 21期

关键词：

D O I：

10.1021/jm030180y

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The binding interactions of the phosphosulfomannan anticancer agent PI-88 (1) with the angiogenic growth factors FGF-1, FGF-2, and VEGF were studied by surface plasmon resonance (SPR) on a BIAcore 3000 biosensor. Compared with heparin, PI-88 has at least 11-fold higher affinity for FGF-1 and at least Mold higher affinity for VEGF, but at least 13-fold lower affinity for FGF-2. To define the structural features of PI-88 that are important for growth factor binding, several analogues, such as dephosphorylated PI-88 and a sulfated pentasaccharide, were prepared. The binding interactions of these analogues with FGF-1, FGF-2, and VEGF were similarly studied by SPR, and structure-activity relationships were determined.

引用

页码：4601 / 4608

页数：8

共 49 条

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