Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors.

doi:10.1038/nature08675

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Article

Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors.

Nature - 28 Jan 2010

Zhang Jianming, Adrián Francisco J, Jahnke Wolfgang, Cowan-Jacob Sandra W, Li Allen G, Iacob Roxana E, Sim Taebo, Powers John, Dierks Christine, Sun Fangxian, Guo Gui-Rong, Ding Qiang, Okram Barun, Choi Yongmun, Wojciechowski Amy, Deng Xianming, Liu Guoxun, Fendrich Gabriele, Strauss André, Vajpai Navratna, Grzesiek Stephan, Tuntland Tove, Liu Yi, Bursulaya Badry, Azam Mohammad, Manley Paul W, Engen John R, Daley George Q, Warmuth Markus, Gray Nathanael S

Abstract excerpt

In an effort to find new pharmacological modalities to overcome resistance to ATP-binding-site inhibitors of Bcr-Abl, we recently reported the discovery of GNF-2, a selective allosteric Bcr-Abl inhibitor. Here, using solution NMR, X-ray crystallography, mutagenesis and hydrogen exchange mass spectrometry, we show that GNF-2 binds to the myristate-binding site of Abl, leading to changes in the structural dynamics...

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PMID: 20072125
DOI: 10.1038/nature08675
PMCID: PMC2901986

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