Strategies for the NMR-based identification and optimization of allosteric protein kinase inhibitors

被引:24
|
作者
Jahnke, W [1 ]
Blommers, MJJ [1 ]
Fernández, C [1 ]
Zwingelstein, C [1 ]
Amstutz, R [1 ]
机构
[1] Novartis Inst Biomed Res, CH-4002 Basel, Switzerland
关键词
D O I
10.1002/cbic.200500100
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Caught coming in the back door. Kinases are important drug targets, and new methods for the identification of novel classes of kinase inhibitors are urgently needed. By using a spin-labeled analogue of adenine (shown as a red star), second-site NMR screening can identify allosteric kinase inhibitors (right) that bind outside of the ATP-binding pocket and might have an interesting selectivity profile. © 2005 Wiley-VCH Verlag GmbH & Co. KGaA.
引用
收藏
页码:1607 / +
页数:5
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