Mutation in the ABL kinase domain is the principal mechanism of imatinib resistance in
patients with chronic myelogenous leukemia. Many mutations favor active kinase …

Structural studies suggest that most point mutations in the BCR-ABL kinase domain cause
resistance to the ABL kinase inhibitor imatinib by impairing the flexibility of the kinase …

Imatinib (Gleevec)(formerly STI571) competitively targets the adenosine 5-triphosphate
(ATP) binding site of the kinase domain of ABL and was recently approved for the treatment …

Protein kinase inhibitors are potent anticancer therapeutics. For example, the Bcr-Abl kinase
inhibitor imatinib decreases mortality for chronic myeloid leukemia by 80%, but 22 to 41% of …

The ABL inhibitor imatinib is a highly effective therapy for patients with chronic myeloid
leukemia. Relapses after an initial response have been observed in some patients, and …

Imatinib, a specific small molecule inhibitor of the Abl kinase, has become the standard drug
therapy for chronic myelogenous leukemia in all phases. More than 80% of newly …

Therapy with ATP-competitive ABL kinase inhibitors, including imatinib (Gleevec), dasatinib
(Sprycel), and nilotinib (Tasigna), has revolutionized the treatment of chronic myeloid …

Imatinib, a small-molecule ABL kinase inhibitor, is a highly effective therapy for early-phase
chronic myeloid leukaemia (CML), which has constitutively active ABL kinase activity owing …

The leukemogenic tyrosine kinase Bcr-Abl contains a highly conserved inhibitor-binding
pocket (IBP), which serves as a binding site for imatinib mesylate. Mutations at the IBP may …

Imatinib mesylate is a selective Bcr-Abl kinase inhibitor, effective in the treatment of chronic
myelogenous leukemia. Most patients in chronic phase maintain durable responses; …