Article
Expanding the diversity of allosteric bcr-abl inhibitors.
Journal of medicinal chemistry - 14 Oct 2010
Deng Xianming, Okram Barun, Ding Qiang, Zhang Jianming, Choi Yongmun, Adrián Francisco J, Wojciechowski Amy, Zhang Guobao, Che Jianwei, Bursulaya Badry, Cowan-Jacob Sandra W, Rummel Gabriele, Sim Taebo, Gray Nathanael S
Abstract excerpt
Inhibition of Bcr-Abl kinase activity by imatinib for the treatment of chronic myeloid leukemia (CML) currently serves as the paradigm for targeting dominant oncogenes with small molecules. We recently reported the discovery of GNF-2 (1) and GNF-5 (2) as selective non-ATP competitive inhibitors of cellular Bcr-Abl kinase activity that target the myristate binding site. Here, we used cell-based structure-activity...
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