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Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of Bcr-Abl positive cells
Abstract
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 92-98% decrease in the number of bcr-abl colonies formed but no inhibition of normal colony formation. This compound may be useful in the treatment of bcr-abl-positive leukemias.
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“Imatinib mesylate, an Abl kinase inhibitor, has been identified as an effective treatment option for p210-BCR-ABL-mediated leukemia (Druker et al., 1996).”
From Rac Guanosine Triphosphatases Represent Integrating Molecular Therapeutic Targets for BCR-ABL-Induced Myeloproliferative Disease (2007) · cites this paper as Druker et al., 1996
In the citing paper
“Imatinib (Gleevec, also known as STI571 or CGP57148), an Abl kinase inhibitor that shows significant activity in all phases of CML and Ph-positive acute leukemias (Druker et al., 2002) by selective induction of apoptosis of p210-BCR-ABL-positive cells (Druker et al., 1996;Deininger et al., 1997;le Coutre et al., 1999)”
From Rac Guanosine Triphosphatases Represent Integrating Molecular Therapeutic Targets for BCR-ABL-Induced Myeloproliferative Disease (2007) · cites this paper as Druker et al., 1996
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Metadata
- Authors
- Druker, B. J., Tamura, S., Buchdunger, E., Ohno, S., Segal, G. M., Fanning, S., Zimmermann, J., & Lydon, N. B.
- Venue
- Nature Medicine
- Published
- 1996-05
- Volume
- 2
- Issue
- 5
- Pages
- 561-566
- ISSN
- 1078-8956
- 1546-170X
- Cited by
- 2,967
- References
- 1
- Language
- en
- Licence
- www.springer.com/tdm (tdm)
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- Druker, B. J., Tamura, S., Buchdunger, E., Ohno, S., Segal, G. M., Fanning, S., Zimmermann, J., & Lydon, N. B. (1996). Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of Bcr-Abl positive cells. Nature Medicine. https://doi.org/10.1038/nm0596-561