Gou Yanzi, Geng Jin, Richards Sarah-Jane, Burns James, Remzi Becer C, Haddleton D M
Science and Technology on Advanced Ceramic Fibers and Composites Laboratory, National University of Defense Technology Changsha, 410073, China.
J Polym Sci A Polym Chem. 2013 Jun 15;51(12):2588-2597. doi: 10.1002/pola.26646. Epub 2013 Mar 13.
Synthetic glycopolymers are important natural oligosaccharides mimics for many biological applications. To develop glycopolymeric drugs and therapeutic agents, factors that control the receptor-ligand interaction need to be investigated. A library of well-defined glycopolymers has been prepared by the combination of copper mediated living radical polymerization and CuAAC click reaction via post-functionalization of alkyne-containing precursor polymers with different sugar azides. Employing Concanavalin A as the model receptor, we explored the influence of the nature and densities of different sugars residues (mannose, galactose, and glucose) on the stoichiometry of the cluster, the rate of the cluster formation, the inhibitory potency of the glycopolymers, and the stability of the turbidity through quantitative precipitation assays, turbidimetry assays, inhibitory potency assays, and reversal aggregation assays. The diversities of binding properties contributed by different clustering parameters will make it possible to define the structures of the multivalent ligands and densities of binding epitopes tailor-made for specific functions in the lectin-ligand interaction. © 2013 Wiley Periodicals, Inc. J. Polym. Sci., Part A: Polym. Chem. 2013, 51, 2588-2597.
合成糖聚合物是许多生物应用中重要的天然寡糖模拟物。为了开发糖聚合物药物和治疗剂,需要研究控制受体-配体相互作用的因素。通过铜介导的活性自由基聚合和CuAAC点击反应,将含炔基的前体聚合物与不同的糖叠氮化物进行后功能化,制备了一系列定义明确的糖聚合物。以伴刀豆球蛋白A为模型受体,我们通过定量沉淀试验、比浊法试验、抑制效力试验和逆转聚集试验,探讨了不同糖残基(甘露糖、半乳糖和葡萄糖)的性质和密度对簇的化学计量、簇形成速率、糖聚合物的抑制效力以及浊度稳定性的影响。不同聚类参数所贡献的结合特性的多样性将使得有可能定义多价配体的结构以及为凝集素-配体相互作用中的特定功能量身定制的结合表位的密度。© 2013威利期刊公司。《聚合物科学杂志》,A部分:聚合物化学2013年,51卷,2588 - 2597页。