Small-molecule screening made simple for a difficult target with a signaling nucleic acid aptamer that reports on deaminase activity

被引:47
作者
Elowe, Nadine H.
Nutiu, Razvan
Allah-Hassani, Abdellah
Cechetto, Jonathan D.
Hughes, Donald W.
Li, Yingfu
Brown, Eric A. [1 ]
机构
[1] McMaster Univ, Dept Biochem & Biomed Sci, Hamilton, ON L8N 3Z5, Canada
[2] McMaster Univ, Dept Chem, Hamilton, ON L8N 3Z5, Canada
关键词
adenosine deaminase; assays; DNA structures; inhibitors; small-molecule screening;
D O I
10.1002/anie.200601695
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Problem child: The application of signaling DNA-aptamer technology to the development and execution of a high-throughput screen for an otherwise problematic target, adenosine deaminase (ADA), is reported. The approach employed a signaling DNA aptamer that reports on adenosine concentration (see scheme). The assay was robust in a screen of more than 44 000 molecules and revealed a new competitive inhibitor of the deaminase. (Chemical Equation Presented). © 2006 Wiley-VCH Verlag GmbH & Co. KGaA.
引用
收藏
页码:5648 / 5652
页数:5
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