The BCR-ABL tyrosine kinase inhibitor imatinib represents the current frontline therapy in
chronic myeloid leukemia. Because many patients develop imatinib resistance, 2 second …

Following the initial success of imatinib as frontline therapy for chronic myeloid leukemia
(CML), several second-generation therapeutics have been developed with increased …

Resistance to the BCR-ABL tyrosine kinase inhibitor imatinib poses a pressing challenge in
treating chronic myeloid leukemia (CML). This resistance is often caused by point mutations …

Dasatinib is a small-molecule kinase inhibitor used for the treatment of imatinib-resistant
chronic myelogenous leukemia (CML). We have analyzed the kinases targeted by dasatinib …

Bcr-Abl inhibitors paved the way of targeted therapy epoch. Imatinib was the first tyrosine
kinase inhibitor to be discovered with high specificity for Bcr-Abl protein resulting from t (9 …

Several cancer treatments are shifting from traditional, time-limited, nonspecific cytotoxic
chemotherapy cycles to continuous oral treatment with specific protein-targeted therapies. In …

As a drug used to treat imatinib-resistant and-intolerant, chronic and advanced phase
chronic myelogenous leukaemia, nilotinib is well characterised as a potent inhibitor of the …

Occurrence of the BCR-ABLT315I gatekeeper mutation is among the most pressing
challenges in the therapy of chronic myeloid leukemia (CML). Several BCR-ABL inhibitors …

The detailed molecular mechanism of action of second-generation BCR–ABL tyrosine
kinase inhibitors, including perturbed targets and pathways, should contribute to rationalized …

Current structural understanding of kinases is largely based on x-ray crystallographic
studies, whereas very little data exist on the conformations and dynamics that kinases adopt …