Article
Novel pyrrolo-1,5-benzoxazepine compounds display significant activity against resistant chronic myeloid leukaemia cells in vitro, in ex vivo patient samples and in vivo.
British journal of cancer - 11 May 2010
Bright S A, McElligott A M, O'Connell J W, O'Connor L, Carroll P, Campiani G, Deininger M W, Conneally E, Lawler M, Williams D C, Zisterer D M
Abstract excerpt
BACKGROUND: Imatinib is a direct and potent inhibitor of the constitutively active tyrosine kinase, breakpoint cluster region-Abelson (Bcr-Abl), which is central to the pathogenesis of chronic myeloid leukaemia (CML) patients. As such, imatinib has become the front-line treatment for CML patients. However, the recent emergence of imatinib resistance, commonly associated with point mutations within the kinase...
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