Imatinib can act as an allosteric activator of Abl kinase

2021 ◽  
pp. 167349
Author(s):  
Tao Xie ◽  
Tamjeed Saleh ◽  
Paolo Rossi ◽  
Darcie Miller ◽  
Charalampos G. Kalodimos
Keyword(s):  
Abl Kinase ◽  
Allosteric Activator

scholarly journals Gleevec Can Act as an Allosteric Activator of ABL Kinase

2018 ◽  
Vol 114 (3) ◽  
pp. 229a
Author(s):  
Tao Xie ◽  
Tamjeed Saleh ◽  
Charalampos G. Kalodimos
Keyword(s):  
Abl Kinase ◽  
Allosteric Activator

BCR-ABL kinase domain mutation analysis in chronic myeloid leukemia patients treated with tyrosine kinase inhibitors: recommendations from an expert panel on behalf of European LeukemiaNet

Blood ◽  
2011 ◽  
Vol 118 (5) ◽  
pp. 1208-1215 ◽  
Author(s):  
Simona Soverini ◽  
Andreas Hochhaus ◽  
Franck E. Nicolini ◽  
Franz Gruber ◽  
Thoralf Lange ◽  
...  
Keyword(s):  
Chronic Myeloid Leukemia ◽  
Tyrosine Kinase ◽  
Tyrosine Kinase Inhibitors ◽  
Mutation Analysis ◽  
Myeloid Leukemia ◽  
Kinase Inhibitors ◽  
Direct Sequencing ◽  
Chronic Phase ◽  
Kinase Domain ◽  
Abl Kinase

AbstractMutations in the Bcr-Abl kinase domain may cause, or contribute to, resistance to tyrosine kinase inhibitors (TKIs) in chronic myeloid leukemia patients. Recommendations aimed to rationalize the use of BCR-ABL mutation testing in chronic myeloid leukemia have been compiled by a panel of experts appointed by the European LeukemiaNet (ELN) and European Treatment and Outcome Study and are here reported. Based on a critical review of the literature and, whenever necessary, on panelists' experience, key issues were identified and discussed concerning: (1) when to perform mutation analysis, (2) how to perform it, and (3) how to translate results into clinical practice. In chronic phase patients receiving imatinib first-line, mutation analysis is recommended only in case of failure or suboptimal response according to the ELN criteria. In imatinib-resistant patients receiving an alternative TKI, mutation analysis is recommended in case of hematologic or cytogenetic failure as provisionally defined by the ELN. The recommended methodology is direct sequencing, although it may be preceded by screening with other techniques, such as denaturing-high performance liquid chromatography. In all the cases outlined within this abstract, a positive result is an indication for therapeutic change. Some specific mutations weigh on TKI selection.

scholarly journals Short-term intense Bcr–Abl kinase inhibition with nilotinib is adequate to trigger cell death in BCR-ABL+ cells

Leukemia ◽  
2009 ◽  
Vol 23 (6) ◽  
pp. 1205-1206 ◽  
Author(s):  
D K Hiwase ◽  
D L White ◽  
V A Saunders ◽  
S Kumar ◽  
J V Melo ◽  
...  
Keyword(s):  
Cell Death ◽  
Short Term ◽  
Kinase Inhibition ◽  
Abl Kinase ◽  
Trigger Cell Death

scholarly journals In vitro Activity of Bcr-Abl Inhibitors AMN107 and BMS-354825 against Clinically Relevant Imatinib-Resistant Abl Kinase Domain Mutants

2005 ◽  
Vol 65 (11) ◽  
pp. 4500-4505 ◽  
Author(s):  
Thomas O'Hare ◽  
Denise K. Walters ◽  
Eric P. Stoffregen ◽  
Taiping Jia ◽  
Paul W. Manley ◽  
...  
Keyword(s):  
Kinase Domain ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Abl Kinase ◽  
Imatinib Resistant

Design, synthesis and biological evaluation of novel acrylamide analogues as inhibitors of BCR–ABL kinase

2012 ◽  
Vol 22 (16) ◽  
pp. 5279-5282 ◽  
Author(s):  
Shuxin Li ◽  
Zhenglin Yao ◽  
Yanjin Zhao ◽  
Wei Chen ◽  
Huijia Wang ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Abl Kinase ◽  
Acrylamide Analogues ◽  
Synthesis And Biological Evaluation

ChemInform Abstract: Potent and Selective Inhibitors of the AbL-Kinase: Phenylaminopyrimidine (PAP) Derivatives.

ChemInform ◽  
2010 ◽  
Vol 28 (20) ◽  
pp. no-no
Author(s):  
J. ZIMMERMANN ◽  
E. BUCHDUNGER ◽  
H. METT ◽  
T. MEYER ◽  
N. B. LYDON
Keyword(s):  
Selective Inhibitors ◽  
Abl Kinase
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