A comparison of biological and calorimetric analyses of multivalent glycodendrimer ligands for concanavalin A
A comparison of biological and calorimetric analyses of multivalent glycodendrimer ligands for concanavalin A
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DOI：
10.1016/s0957-4166(99)00589-3
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发表时间：
2000-01-28
影响因子：
--
通讯作者：
Toone, EJ
中科院分区：
文献类型：
--
作者：
Corbell, JB;Lundquist, JJ;Toone, EJ
簇糖苷效应-观察到多价糖苷与其多价蛋白质受体结合的表观亲和力大于仅基于化合价可以合理化的亲和力，这是目前公认的现象。作为一个持续的努力，以提供一个分子基础的簇糖苷效应的一部分，我们在这里报告的两个系列的甘露糖基化的树突状配体的合成和它们的性能在一系列的竞争性和非竞争性结合试验，包括hemeagglutamine抑制（HIA），酶联凝集素测定（ELLA）和等温滴定微量热法（ITC）。第一系列配体含有半刚性甘氨酰甘氨酸间隔物，并且在任何结合研究中均未显示出显著的性能增强。第二系列的配体含有柔性四甘醇间隔基;这些配体在HIA中在四价和六价水平均显示出显著的增强（IC 50 =3和IC 50 = 4）。
The cluster glycoside effect - the observation that multivalent glycosides bind to their polyvalent protein receptors with apparent affinities greater than those that can be rationalized solely on the basis of valency is by now a well established phenomenon. As part of a continuing effort to provide a molecular basis for the cluster glycoside effect, we report here the synthesis of two series of mannosylated dendritic ligands and their performance in a range of competitive and non-competitive binding assays, including hemeagglutination inhibition (HIA), enzyme-linked lectin assays (ELLA) and isothermal titration microcalorimetry (ITC). The first series of ligands contained a semi-rigid glycylglycine spacer and showed no significant performance enhancement in any binding studies. The second series of ligands contained a flexible tetraethylene glycol spacer; these ligands showed marked enhancements at tetravalent and hexavalent levels in both HIA (IC50=3 and