Although inhibitors directed against the ATP-binding site of the kinase, such as imatinib (Glivec/Gleevec ... a selective allosteric inhibitor of BCR–ABL, GNF-5, that cooperates with ATP ...

Point mutations within the Abl kinase domain that interfere with imatinib binding are the most ... Abl Tyrosine Kinase Inhibitors for Overriding Bcr-Abl/T315I: From the Second to Third Generation ...

More than 95% of chronic myeloid leukemia (CML) and 20%-30% of acute lymphoblastic leukemia (ALL) patients express the fusion ...

Therefore, it is necessary to develop more effective Abl TKIs that are both orally bioavailable and more potent than imatinib in blocking Bcr–Abl kinase activity, including variants with point ...

In experiments that today would typically be pursued first by RNA interference, Brian Druker and his colleagues showed that imatinib inhibits BCR-ABL kinase activity and selectively impairs the ...

A new approach helps examine the proportion of cancerous and healthy stem cells in patients with chronic myeloid leukemia and how this influences treatment outcomes.

Targeted therapy revolutionized cancer treatment, with gene fusions leading the way when the FDA approved imatinib in 2001 to ...