Departamento de Química Orgánica, Facultad de Química, Universidad de Sevilla, Apartado 1203, E-41012 Sevilla, Spain.
Org Biomol Chem. 2010 Apr 21;8(8):1849-60. doi: 10.1039/b920048g.
A versatile synthetic procedure to construct series of high- and low-density homo- and heteroglycoclusters is reported. The binding properties of these synthetic multivalent glycoconjugates to concanavalin A (Con A), a model lectin, have been assessed by using a range of competitive and non-competitive binding assays including enzyme-linked lectin assays (ELLA), isothermal titration microcalorimetry (ITC) and surface plasmon resonance (SPR). In all cases, highly dense glycoclusters showed a substantial amplification of the lectin-binding strength in comparison with low-density counterparts. Interestingly, highly-dense glycoligand presentations, regardless of their homo- or heteroglycoligand pattern, furnished similar Con A binding properties, supporting the existence of a synergic effect (heterocluster effect) due to secondary interactions of "non-active" structural motifs in the presence of a certain density of "active" glycoligands.
报道了一种通用的合成方法，用于构建一系列高密度和低密度的同型和异型寡糖簇。通过使用一系列竞争性和非竞争性结合测定法，包括酶联凝集素测定法（ELLA）、等温滴定量热法（ITC）和表面等离子体共振（SPR），评估了这些合成的多价糖缀合物与伴刀豆球蛋白 A（Con A），一种模型凝集素的结合特性。在所有情况下，与低密度对应物相比，高密度糖缀合物显示出对凝集素结合强度的显著增强。有趣的是，高密度糖配体呈现方式，无论其同型或异型寡糖配体模式如何，都提供了相似的 Con A 结合特性，这支持了协同效应（杂合簇效应）的存在，这是由于在一定密度的“活性”糖配体存在下，“非活性”结构基序的次级相互作用所致。
