Chronic Myeloid Leukemia (CML) is a clonal disease characterized by the presence of the
Philadelphia (Ph+) chromosome and its oncogenic product, BCR-ABL, a constitutively active …

Bosutinib, a dual Src/Abl tyrosine kinase inhibitor (TKI), has shown potent activity against
chronic myeloid leukemia (CML). This phase 1/2 study evaluated the efficacy and safety of …

Therapies that target BCR-ABL in chronic myeloid leukemia, including imatinib, dasatinib
and nilotinib, have dramatically improved patient outcome. BCR-ABL mutations, however …

Preclinical studies of BCR-ABL mutation sensitivity to nilotinib or dasatinib suggested that
the majority would be sensitive. Correspondingly, the initial clinical trials demonstrated …

The majority of kinase inhibitors developed to date are competitive inhibitors that target the
ATP binding site; however, recent crystal structures of Gleevec®(imatinib mesylate, STI571 …

Inactive conformations of protein kinase catalytic domains where the DFG motif has a “DFG-
out” orientation and the activation loop is folded present a druggable binding pocket that is …

Background BCR-ABL kinase domain mutations are infrequently detected in newly
diagnosed chronic-phase chronic myeloid leukemia (CML) patients. Recent studies indicate …

Chronic myeloid leukemia (cml) results from expression of the constitutive tyrosine kinase
activity of the Bcr-Abl oncoprotein. Imatinib, a tyrosine kinase inhibitor (tki), is highly effective …

In patients with chronic myeloid leukemia (CML), disease in the initial chronic phase (CP)
and subsequent progression are driven by the oncogenic activity of the BCR–ABL fusion …

Eur J Clin Invest 2010; 40 (10): 918–931 Abstract Chronic myeloid leukaemia (CML) is a
haematopoietic neoplasm characterised by the BCR/ABL1 oncoprotein. In chronic phase …