Article
Selective cytotoxic mechanism of GTP-14564, a novel tyrosine kinase inhibitor in leukemia cells expressing a constitutively active Fms-like tyrosine kinase 3 (FLT3).
The Journal of biological chemistry - 29 Aug 2003
Murata Ken, Kumagai Hidetoshi, Kawashima Toshiyuki, Tamitsu Kaori, Irie Mariko, Nakajima Hideaki, Suzu Shinya, Shibuya Masabumi, Kamihira Shimeru, Nosaka Tetsuya, Asano Shigetaka, Kitamura Toshio
Abstract excerpt
The receptor tyrosine kinase FLT3 is constitutively activated by an internal tandem duplication (ITD) mutation within the juxtamembrane domain in 20-30% of patients with acute myeloid leukemia. In this study, we identified GTP-14564 as a specific kinase inhibitor for ITD-FLT3 and investigated the molecular basis of its specificity. GTP-14564 inhibited the growth of interleukin-3-independent Ba/F3 expressing...
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