Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of Bcr-Abl positive cells.
basic_science · Level V
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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.
Medical subject headings
- Enzyme Inhibitors
- Fusion Proteins, bcr-abl
- Leukemia, Myelogenous, Chronic, BCR-ABL Positive
- Piperazines
- Protein-Tyrosine Kinases
- Proto-Oncogene Proteins c-abl
- Pyrimidines