A Type-II Kinase Inhibitor Capable of Inhibiting the T315I “Gatekeeper” mutant of Bcr-Abl

The second generation of Bcr-Abl inhibitors nilotinib, dasatinib, and bosutinib developed to override imatinib resistance are not active against the T315I ‘gatekeeper’ mutation. Here we describe a Type-II T315I inhibitor GNF-7, based upon a 3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one scaffold whic...

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Main Authors: Choi, Hwan Geun, Ren, Pingda, Adrian, Francisco, Sun, Fangxian, Lee, Hyun Soo, Wang, Xia, Ding, Qiang, Zhang, Guobao, Zhang, Yongping, Liu, Yi, Tuntland, Tove, Warmuth, Markus, Manley, Paul W., Mestan, Jürgen, Gray, Nathanael S, Sim, Taebo
格式: Artigo
語言:Inglês
出版: 2010
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在線閱讀:https://ncbi.nlm.nih.gov/pmc/articles/PMC4134510/
https://ncbi.nlm.nih.gov/pubmed/20604564
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm901808w
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