Article
Inhibition of wild-type and mutant Bcr-Abl by AP23464, a potent ATP-based oncogenic protein kinase inhibitor: implications for CML.
Blood - 15 Oct 2004
O'Hare Thomas, Pollock Roy, Stoffregen Eric P, Keats Jeffrey A, Abdullah Omar M, Moseson Erika M, Rivera Victor M, Tang Hao, Metcalf Chester A, Bohacek Regine S, Wang Yihan, Sundaramoorthi Raji, Shakespeare William C, Dalgarno David, Clackson Tim, Sawyer Tomi K, Deininger Michael W, Druker Brian J
Abstract excerpt
The deregulated, oncogenic tyrosine kinase Bcr-Abl causes chronic myeloid leukemia (CML). Imatinib mesylate (Gleevec, STI571), a Bcr-Abl kinase inhibitor, selectively inhibits proliferation and promotes apoptosis of CML cells. Despite the success of imatinib mesylate in the treatment of CML, resistance is observed, particularly in advanced disease. The most common imatinib mesylate resistance mechanism involves...
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