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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Hoofdauteurs: 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
Formaat: Artigo
Taal:Inglês
Gepubliceerd in: 2010
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Article
Online toegang: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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