STI-571 must select for drug-resistant cells but ‘no cell breathes fire out of its nostrils like a dragon’
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چکیده
منابع مشابه
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The inadvertent activation of the Abelson tyrosine kinase (Abl) causes chronic myelogenous leukemia (CML). A small-molecule inhibitor of Abl (STI-571) is effective in the treatment of CML. We report the crystal structure of the catalytic domain of Abl, complexed to a variant of STI-571. Critical to the binding of STI-571 is the adoption by the kinase of an inactive conformation, in which a cent...
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Interactions between the Bcr-Abl kinase inhibitor STI-571 (imatinib mesylate) and a novel microtubule-targeting agent (MTA), pyrrolo-1,5-benzoxazepine (PBOX)-6, were investigated in STI-571-sensitive and -resistant human chronic myeloid leukemia (CML) cells. Cotreatment of PBOX-6 with STI-571 induced significantly more apoptosis in Bcr-Abl-positive CML cell lines (K562 and LAMA-84) than either ...
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STI-571, a new Abl tyrosine kinase inhibitor recently approved by the Food and Drug Administration, is highly effective in treating the early stages of chronic myeloid leukemia (CML), but remissions induced in advanced phases tend to be relatively short-lived, an observation that suggests the development of de novo resistance to the drug (1, 2). Gorre et al. (3) showed that “acquired” resistanc...
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ژورنال
عنوان ژورنال: Leukemia
سال: 2002
ISSN: 0887-6924,1476-5551
DOI: 10.1038/sj.leu.2402409