Phosphorylation of the ATP-binding loop directs oncogenicity of drug-resistant BCR-ABL mutants

BJ Skaggs, ME Gorre, A Ryvkin… - Proceedings of the …, 2006 - National Acad Sciences
The success of targeting kinases in cancer with small molecule inhibitors has been
tempered by the emergence of drug-resistant kinase domain mutations. In patients with …

Bcr-Abl resistance screening predicts a limited spectrum of point mutations to be associated with clinical resistance to the Abl kinase inhibitor nilotinib (AMN107)

N Von Bubnoff, PW Manley, J Mestan, J Sanger… - Blood, 2006 - ashpublications.org
In advanced-phase chronic myeloid leukemia (CML), resistance to imatinib mesylate is
associated with point mutations in the BCR-ABL kinase domain. A new generation of potent …

New tyrosine kinase inhibitors in the treatment of chronic myeloid leukemia

S Kimura, E Ashihara… - Current pharmaceutical …, 2006 - ingentaconnect.com
Imatinib mesylate, Abl tyrosine kinase inhibitor, has improved the treatment of Bcr-Abl-
positive leukemia such as chronic myeloid leukemia (CML) and Philadelphia chromosome …

The second generation of BCR-ABL tyrosine kinase inhibitors

T Tauchi, K Ohyashiki - International journal of hematology, 2006 - Springer
Imatinib was developed as the first molecularly targeted therapy to specifically inhibit the
BCR-ABL kinase in Philadelphia chromosome (Ph)-positive chronic myeloid leukemia …

Imatinib mesylate resistance through BCR-ABL independence in chronic myelogenous leukemia

NJ Donato, JY Wu, J Stapley, H Lin, R Arlinghaus… - Cancer research, 2004 - AACR
Imatinib mesylate (IM) binds to the BCR-ABL protein, inhibiting its kinase activity and
effectively controlling diseases driven by this kinase. IM resistance has been associated with …

Novel targeted therapies to overcome imatinib mesylate resistance in chronic myeloid leukemia (CML)

C Walz, M Sattler - Critical reviews in oncology/hematology, 2006 - Elsevier
Imatinib mesylate (Gleevec) was developed as the first molecularly targeted therapy that
specifically inhibits the BCR–ABL tyrosine kinase activity in patients with Philadelphia …

Hematologic and Cytogenetic Responses in Imatinib-Resistant Chronic Phase Chronic Myeloid Leukemia Patients Treated with the Dual SRC/ABL Kinase Inhibitor …

CL Sawyers, NP Shah, HM Kantarjian, N Donato… - Blood, 2004 - Elsevier
Disease relapse in CML patients treated with imatinib is often associated with mutations in
the BCR-ABL gene that interfere with the ability of imatinib to block BCR-ABL kinase activity …

Denaturing-HPLC-based assay for detection of ABL mutations in chronic myeloid leukemia patients resistant to Imatinib

S Soverini, G Martinelli, M Amabile, A Poerio… - Clinical …, 2004 - academic.oup.com
Background: Despite the efficacy of the BCR-ABL tyrosine kinase inhibitor Imatinib mesylate
for the treatment of chronic myeloid leukemia (CML), resistance has been observed in a …

[HTML][HTML] Development of asciminib, a novel allosteric inhibitor of BCR-ABL1

D Réa, TP Hughes - Critical Reviews in Oncology/Hematology, 2022 - Elsevier
Chronic myeloid leukemia (CML) is driven by a translocation event between chromosomes 9
and 22, leading to the formation of a constitutively active BCR-ABL1 oncoprotein. Approved …

Novel agents in CML therapy: tyrosine kinase inhibitors and beyond

JV Melo, C Chuah - ASH Education Program Book, 2008 - ashpublications.org
The emergence of resistance to imatinib has become a significant problem despite the
remarkable clinical results achieved with this tyrosine kinase inhibitor in the treatment of …