Identification of compounds with binding affinity to proteins via magnetization transfer from bulk water

Identification of compounds with binding affinity to proteins via magnetization transfer from bulk water
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DOI:
10.1023/a:1008354229396
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发表时间:
2000-09-01
影响因子:
2.7
通讯作者:
Sundström, M
Sundström, M
中科院分区:
生物学3区
文献类型:
--
作者:
Dalvit, C;Pevarello, P;Sundström, M

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一个强大的筛选NMR方法(WaterLOGSY),从散装水的磁化转移的基础上,用于识别与目标生物分子(蛋白质,RNA和DNA片段)相互作用的化合物。该方法有效地利用了水磁化的大水库。该技术的高灵敏度减少了筛选所需的生物分子和配体的量,这构成了通过NMR对大型化合物库进行高通量筛选的重要要求。应用该方法对细胞周期蛋白依赖性激酶2(cdk2)蛋白的化合物混合物。
A powerful screening by NMR methodology (WaterLOGSY), based on transfer of magnetization from bulk water, for the identification of compounds that interact with target biomolecules (proteins, RNA and DNA fragments) is described. The method exploits efficiently the large reservoir of H2O magnetization. The high sensitivity of the technique reduces the amount of biomolecule and ligands needed for the screening, which constitutes an important requirement for high throughput screening by NMR of large libraries of compounds. Application of the method to a compound mixture against the cyclin-dependent kinase 2 (cdk2) protein is presented.