Synthesis and biological evaluation of a heparin-like hexasaccharide with the structural motifs for binding to FGF and FGFR
Synthesis and biological evaluation of a heparin-like hexasaccharide with the structural motifs for binding to FGF and FGFR
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DOI：
10.1002/ejoc.200400799
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发表时间：
2005-04-29
影响因子：
2.8
通讯作者：
Martin-Lomas, M
中科院分区：
文献类型：
--
作者：
de Paz, JL;Martin-Lomas, M
基于晶体学数据，设计了一种肝素样六糖结构(2)，该结构包含与酸性成纤维细胞生长因子（FGF-1）及其受体（FGFR）相互作用的两个三糖序列。该六糖已通过完全立体选择性模块化方法有效合成，并通过测定其刺激fgf -1诱导的有丝分裂活性的能力进行了生物学评估。发现该分子没有明显的FGF-1激活作用。(c) Wiley-VCH Verlag GmbH & Co. KGaA
A heparin-like hexasaccharide structure (2) containing the two trisaccharide sequences that interact with acidic fibroblast growth factor (FGF-1) and with its receptor (FGFR) has been designed on the basis of crystallographic data. This hexasaccharide has been effectively synthesized by a completely stereoselective modular approach and biologically evaluated by determination of its capacity to stimulate FGF-1-induced mitogenic activity. It was found that this molecule did not show an appreciable FGF-1 activating effect. (c) Wiley-VCH Verlag GmbH & Co. KGaA.