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一种基于配体的核磁共振筛选方法,用于鉴定和表征淀粉样肽聚集的抑制剂和促进剂。

A Ligand-Based NMR Screening Approach for the Identification and Characterization of Inhibitors and Promoters of Amyloid Peptide Aggregation.

作者信息

Dalvit Claudio, Santi Sara, Neier Reinhard

机构信息

Department of Chemistry, University of Neuchatel, Avenue de Bellevaux 51, 2000, Neuchatel, Switzerland.

出版信息

ChemMedChem. 2017 Sep 7;12(17):1458-1463. doi: 10.1002/cmdc.201700319. Epub 2017 Aug 7.

Abstract

Over the years a significant amount of effort has been put into the development of rapid and reliable methods to monitor the aggregation dynamics of the β amyloid peptide in real time. We present an alternative approach based on a suitable reporter or spy molecule and three different NMR experiments: WaterLOGSY, H selective T filter, and F T filter, for monitoring the initial self-aggregation process kinetics of the β amyloid peptide and identifying molecules that retard or accelerate the self-aggregation process. Although the proposed method is not a high-throughput assay, it avoids problems associated with interference events that are sometimes observed in fluorescence-based assays.

摘要

多年来,人们投入了大量精力来开发快速可靠的方法,以实时监测β淀粉样肽的聚集动力学。我们提出了一种基于合适的报告分子或间谍分子以及三种不同核磁共振实验(WaterLOGSY、氢选择性T滤波器和氟T滤波器)的替代方法,用于监测β淀粉样肽的初始自聚集过程动力学,并识别阻碍或加速自聚集过程的分子。虽然所提出的方法不是高通量分析方法,但它避免了基于荧光的分析中有时会观察到的干扰事件相关问题。

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