Increased SPR-sensitivity enables fragment screening and kinetic characterization at lower surface densities

U. Roder
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Abstract

Aldose Reductase (AR) is a 36 kDa NADPHdependent enzyme involved in glucose metabolism It is a potential target for the prevention of diabetic complications. 3D structural analysis had shown that six selected compounds could be divided into two groups based on mode of action; one group left the hydrophobic pocket closed and the other group opened the binding pocket. The purpose of this study was to elucidate if the difference between the two groups is reflected in their binding kinetics. Introduction
增加的spr灵敏度可以在较低表面密度下进行碎片筛选和动力学表征
醛糖还原酶(AR)是一种36kda的nadph依赖性酶,参与葡萄糖代谢,是预防糖尿病并发症的潜在靶点。三维结构分析表明,六个选定的化合物可以根据作用方式分为两类;一组保持疏水口袋关闭,另一组打开结合口袋。本研究的目的是阐明两组之间的差异是否反映在它们的结合动力学上。介绍
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