Chandra J, Tracy J, Loegering D, Flatten K, Verstovsek S, Beran M, Gorre M, Estrov Z, Donato N, Talpaz M, Sawyers C, Bhalla K, Karp J, Sausville E, Kaufmann SH
Blood. 2005 Nov 15;
The bcr/abl kinase has been targeted for the treatment of chronic myelogenous leukemia (CML) by imatinib mesylate. While imatinib has been extremely effective for chronic phase CML, blast crisis CML and Ph+ ALL are often resistant. In particular, mutation of the T315 residue in the bcr/abl activation loop renders cells highly resistant to imatinib and to second-generation kinase inhibitors such as BMS354825 or AMN107. Adaphostin is a tyrphostin that was originally intended to inhibit the bcr/abl kinase by competing with its peptide substrates. Recent findings have, in addition, implicated the capacity to generate reactive oxygen species (ROS) in the cytotoxic mechanism of adaphostin. I
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Posted by Rob to CML Newswire: Medical And Technical News On Chronic Myelogenous Leukemia at 12/17/2005 05:04:28 PM
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