Targeting wild-type and T315I Bcr-Abl by combining allosteric with ATP-site inhibitors

In an effort to find new pharmacological modalities to overcome resistance to ATP-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...

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Hauptverfasser: 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, Andre, 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.
Format: Artigo
Sprache:Inglês
Veröffentlicht: 2010
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Article
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC2901986/
https://ncbi.nlm.nih.gov/pubmed/20072125
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1038/nature08675
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