The tyrosine kinase inhibitor CGP57148B selectively inhibits the growth of BCR-ABL–positive cells

MWN Deininger, JM Goldman… - Blood, The Journal of …, 1997 - ashpublications.org
… to inhibit the tyrosine kinase of ABL and BCR-ABL with high selectivity 13 ; only the tyrosine
kinases … = 0.25 μmol/L for BCR-ABL autophosphorylation). The data indicated activity against …

BCR-ABL tyrosine kinase inhibitors in the treatment of Philadelphia chromosome positive chronic myeloid leukemia: a review

X An, AK Tiwari, Y Sun, PR Ding, CR Ashby Jr… - Leukemia research, 2010 - Elsevier
… that selectively inhibit the aberrant BCR-ABL tyrosine kinase. … ), is the first BCR-ABL tyrosine
kinase inhibitor (TKI) to be … the ABL kinase domain or overexpression of BCR-ABL could …

Bcr-Abl tyrosine kinase inhibitors: a patent review

A Desogus, S Schenone, C Brullo… - Expert Opinion on …, 2015 - Taylor & Francis
Introduction: Breakpoint cluster region Abelson (Bcr-Abl) tyrosine kinase (TK) is a constitutively
activated cytoplasmic TK and is the underlying cause of chronic myeloid leukemia (CML). …

Inhibition of the Bcr-Abl tyrosine kinase as a therapeutic strategy for CML

BJ Druker - Oncogene, 2002 - nature.com
… Based on this, we developed an assay for Bcr-Abl kinase inhibition, by examining the
relative proportion of Crkl isoforms before and during treatment. These assays showed that a …

The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib

O Hantschel, U Rix, U Schmidt… - Proceedings of the …, 2007 - National Acad Sciences
… a kinase inhibitor with a broader specificity that may target additional kinases upstream or
downstream of Bcr-Abl, thereby decreasing the overall oncogenic potency of the Bcr-Abl effect …

Targeting the BCR-ABL tyrosine kinase in chronic myeloid leukemia

JM Goldman, JV Melo - New England Journal of Medicine, 2001 - Mass Medical Soc
… The two reports by Druker and colleagues in this issue of the Journal, 5,6 which document
the clinical efficacy of the BCR-ABL tyrosine kinase inhibitor STI571 in CML, must be …

Efficacy and safety of a specific inhibitor of the BCR-ABL tyrosine kinase in chronic myeloid leukemia

BJ Druker, M Talpaz, DJ Resta, B Peng… - … England Journal of …, 2001 - Mass Medical Soc
tyrosine kinase activity of the protein is required for its oncogenic activity. For these reasons,
an inhibitor of the BCR-ABL tyrosine kinase … screening for tyrosine kinase inhibitors and its …

Lessons learned from the development of an abl tyrosine kinase inhibitor for chronic myelogenous leukemia

BJ Druker, NB Lydon - The Journal of clinical investigation, 2000 - Am Soc Clin Investig
Bcr-Abl tyrosine kinase as an ideal target for validating the clinical utility of protein kinase
inhibitors… Through these efforts, we believe that the Bcr-Abl kinase inhibitor story will be but the …

Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of BcrAbl positive cells

BJ Druker, S Tamura, E Buchdunger, S Ohno… - Nature medicine, 1996 - nature.com
inhibit the Abl protein tyrosine kinase, was evaluated for its effects on cells containing the
BcrAbl fusion protein… is that with the tyrosine kinase inhibitor, Bcr-Abl protein is still present, but …

Flying under the radar: the new wave of BCRABL inhibitors

A Quintás-Cardama, H Kantarjian… - Nature Reviews Drug …, 2007 - nature.com
… In this respect, the remarkable clinical success of the ABL tyrosine kinase inhibitor (TKI) 4,5
imatinib mesylate (formerly STI571 or CGP 5148B; Gleevec, Novartis) in the treatment of …