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Screening Slow Tight-Binding Glycosidase Inhibitors Using Nanoparticle Immobilized Enzymes

机译:使用纳米颗粒固定化酶筛选缓慢紧密结合的糖苷酶抑制剂

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Glycosidase inhibitors have shown great medicinal and pharmaceutical values as exemplified by therapeutic treatment of influenza virus and non-insulin-dependent diabetes. Some of these enzymes have been considered as important targets for therapeutic development. However, the traditional methods for screening potential inhibitors have been a labor-intensive process. Recent developments on the mass spectrometry had greatly span the possibility of full protein characterization, and even extended to include investigation on noncovalent biomolecular interactions such as many enzyme/substrate and/or inhibitors complexes. However, there are several limitations of the MS-based assay for the slow-tight binding inhibitors. This study is to develop a inhibitor assay based on the mass spectrometry (MS) and nanoparticle immobilized enzyme for the fast screening of subpicomolar slow tight-binding inhibitor of glycosidase.
机译:糖苷酶抑制剂显示出良好的药物和药物值,如受流感病毒和非胰岛素依赖性糖尿病的治疗方法所示。其中一些酶被认为是治疗发育的重要目标。然而,用于筛选潜在抑制剂的传统方法是劳动密集型过程。近期质谱仪的发展极大地跨越了全蛋白表征的可能性,甚至扩展到包括对非共价生物分子相互作用的研究,例如许多酶/衬底和/或抑制剂配合物。然而,对于缓慢紧密结合抑制剂,基于MS的测定存在若干局限性。该研究是基于质谱(MS)和纳米颗粒固定化酶进行抑制剂测定,用于快速筛选糖苷酶的亚哌咪唑慢密粘剂抑制剂。

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