Abl inhibitor BMS354825 binding mode in Abelson kinase revealed by molecular docking studies

C Gambacorti-Passerini, M Gasser, S Ahmed… - Leukemia, 2005 - nature.com
A new SRC-Abl dual inhibitor, BMS354825, has recently been presented as a possible tool
to overcome resistance to imatinib in neoplasias caused by oncogenic variants of the …

Mechanisms of resistance to ABL kinase inhibition in chronic myeloid leukemia and the development of next generation ABL kinase inhibitors

AB Patel, T O'Hare… - Hematology/Oncology …, 2017 - hemonc.theclinics.com
Every year, more than 8000 new cases of chronic myeloid leukemia (CML) are diagnosed in
the United States. 1 BCR-ABL1, a fusion protein kinase derived from a reciprocal …

Molecular mechanisms of resistance to tyrosine kinase inhibitors

M Yaghmaie, CCS Yeung - Current Hematologic Malignancy Reports, 2019 - Springer
Abstract Purpose of Review Chronic myeloid leukemia (CML) patients with constitutive
activity of BCR-ABL1 oncoprotein frequently derive significant clinical benefits from tyrosine …

The specificity of asciminib, a potential treatment for chronic myeloid leukemia, as a myristate-pocket binding ABL inhibitor and analysis of its interactions with mutant …

PW Manley, L Barys, SW Cowan-Jacob - Leukemia research, 2020 - Elsevier
Asciminib is a potent, orally bioavailable, investigational drug that specifically and potently
inhibits the tyrosine kinase activity of native ABL1, together with that of the chimeric BCR …

Inhibitors of the Abl kinase directed at either the ATP-or myristate-binding site

D Fabbro, PW Manley, W Jahnke, J Liebetanz… - … et Biophysica Acta (BBA …, 2010 - Elsevier
The ATP-competitive inhibitors dasatinib and nilotinib, which bind to catalytically different
conformations of the Abl kinase domain, have recently been approved for the treatment of …

The allosteric inhibitor ABL001 enables dual targeting of BCR–ABL1

AA Wylie, J Schoepfer, W Jahnke, SW Cowan-Jacob… - Nature, 2017 - nature.com
Chronic myeloid leukaemia (CML) is driven by the activity of the BCR–ABL1 fusion
oncoprotein. ABL1 kinase inhibitors have improved the clinical outcomes for patients with …

Contribution of ABL kinase domain mutations to imatinib resistance in different subsets of Philadelphia-positive patients: by the GIMEMA Working Party on Chronic …

S Soverini, S Colarossi, A Gnani, G Rosti… - Clinical Cancer …, 2006 - AACR
Purpose: ABL kinase domain mutations have been implicated in the resistance to the BCR-
ABL inhibitor imatinib mesylate of Philadelphia-positive (Ph+) leukemia patients …

BCR-ABL kinase domain mutations in chronic myeloid leukemia: not quite enough to cause resistance to imatinib therapy?

T Lange, B Park, SG Willis, MW Deininger - Cell Cycle, 2005 - Taylor & Francis
Patients with chronic myeloid leukemia (CML) treated with imatinib in early chronic phase
tend to have durable remissions, but there is a high rate of relapse in patients with advanced …

BCR-ABL mutants spread resistance to non-mutated cells through a paracrine mechanism

J Liu, S Joha, T Idziorek, S Corm, D Hetuin, N Philippe… - Leukemia, 2008 - nature.com
Patients with chronic myeloid leukemia who become resistant to the Abl kinase inhibitor
imatinib can be treated with dasatinib. This sequential treatment can lead to BCR-ABL …

Resistance mutations in CML and how we approach them

S Soverini - Hematology, 2023 - ashpublications.org
Among the variety of resistance mechanisms that may underlie a non-optimal response to
tyrosine kinase inhibitor (TKI) therapy in chronic myeloid leukemia patients, secondary point …