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首页> 外文期刊>Chemistry: A European journal >The multivalent effect in glycosidase inhibition: Probing the influence of architectural parameters with cyclodextrin-based iminosugar click clusters
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The multivalent effect in glycosidase inhibition: Probing the influence of architectural parameters with cyclodextrin-based iminosugar click clusters

机译：多价抑制糖苷酶的作用：用基于环糊精的亚氨基糖点击簇探索建筑参数的影响

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摘要

In contrast to most lectins, glycosidases may appear to be unpromising targets for multivalent binding because they display only a single active site. To explore the potential of multivalency on glycosidase inhibition, unprecedented cyclodextrin-based iminosugar conjugates have been designed and prepared. The synthesis was performed by way of Cu~I-catalyzed azide-alkyne cycloaddition reaction under microwave activation between propargylated multivalent β-cyclodextrins and an azide-armed N-alkyl 1-deoxynojirimycin derivative. Evaluation with a panel of glycosidases of this new class of glycomimetic clusters revealed the strongest affinity enhancement observed to date for a multivalent glycosidase inhibitor, with binding enhancement up to four orders of magnitude over the corresponding monovalent ligand for α-mannosidase. These results demonstrate that the multivalency concept extends beyond carbohydrate-lectin recognition processes to glycomimetic-enzyme inhibition.
机译：与大多数凝集素相反，糖苷酶可能似乎是多价结合的目标，因为它们仅显示单个活性位点。为了探索多价抑制糖苷酶的潜力，已经设计和制备了前所未有的基于环糊精的亚氨基糖缀合物。在微波活化的情况下，在丙基活化的多价β-环糊精与叠氮化物武装的N-烷基1-脱氧野rim霉素衍生物之间通过Cu-I催化的叠氮化物-炔烃环加成反应进行合成。用该类新型糖模拟物簇的糖苷酶评估，发现迄今观察到的多价糖苷酶抑制剂的亲和力最强，与α-甘露糖苷酶的相应单价配体相比，结合增强高达四个数量级。这些结果表明，多价概念从碳水化合物-凝集素识别过程扩展到了糖模拟酶的抑制。

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