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

来源：

CHEMBIOCHEM | 2005年 / 6卷 / 09期

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

页码：1607 / +

页数：5

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