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

@article{Druker1996EffectsOA,
  title={Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of Bcr–Abl positive cells},
  author={Brian J. Druker and S Tamura and Elisabeth Buchdunger and Sayuri Ohno and Gerald M. Segal and Sean W. Fanning and J{\"u}rg Zimmermann and Nicholas Lydon},
  journal={Nature Medicine},
  year={1996},
  volume={2},
  pages={561-566}
}
The bcr–abl oncogene, present in 95% of patients with chronic myelogenous leukemia (CML), has been implicated as the cause of this disease. A compound, designed to inhibit the Abl protein tyrosine kinase, was evaluated for its effects on cells containing the Bcr–Abl fusion protein. Cellular proliferation and tumor formation by Bcr–Abl–expressing cells were specifically inhibited by this compound. In colony–forming assays of peripheral blood or bone marrow from patients with CML, there was a 92… 
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TLDR
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TLDR
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TLDR
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TLDR
It is proposed that secondary antiapoptotic signals are entirely responsible for the resistance of Bcr-Abl-positive cells, which are extremely resistant to apoptosis in the absence of tyrosine-kinase activity.
The tyrosine kinase inhibitor CGP57148B selectively inhibits the growth of BCR-ABL-positive cells.
TLDR
CGP57148B, a 2-phenylaminopyrimidine derivative, has been shown to selectively inhibit the tyrosine kinase of ABL and BCR-ABL and it is concluded that this new agent may have significant therapeutic applications.
Mechanisms of Transformation by the BCR/ABL Oncogene
TLDR
Mechanisms of transformation by the BCR/ABL oncogene and opportunities for clin-ical intervention with specific signal transduction inhibitors such as STI-571 in CML are described.
c-Kit Receptor Tyrosine Kinases Characterization of Potent Inhibitors of the Bcr-Abl and the Updated
TLDR
These compounds are potent inhibitors of both the Bcr-Abl and c-kit receptor tyrosine kinases and deserve further study as potential treatments for both CML and for diseases in which c-Kit has a role.
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