Article
Uniform sensitivity of FLT3 activation loop mutants to the tyrosine kinase inhibitor midostaurin.
Blood - 15 Dec 2007
Barry Elly V, Clark Jennifer J, Cools Jan, Roesel Johannes, Gilliland D Gary
Abstract excerpt
Small molecule inhibitors that target fms-like tyrosine kinase 3 (FLT3)-activating mutations have potential in the treatment of leukemias. However, certain mutations can simultaneously activate the tyrosine kinase, and confer resistance to small molecule inhibitors. We therefore tested the sensitivity of 8 FLT3 activation loop mutants to midostaurin. Each mutant conferred IL-3 factor-independent proliferation to...
Topics
- Animals
- Cell Line
- Cell Proliferation
- Extracellular Signal-Regulated MAP Kinases
- Mice
- Mutation
- Phosphorylation
- Protein Kinase Inhibitors
- STAT5 Transcription Factor
- Staurosporine
- Transduction, Genetic