Article
Constitutive activation of c-kit by the juxtamembrane but not the catalytic domain mutations is inhibited selectively by tyrosine kinase inhibitors STI571 and AG1296.
International journal of hematology - 1 Dec 2002
Ueda Shuji, Ikeda Hirokazu, Mizuki Masao, Ishiko Jun, Matsumura Itaru, Tanaka Hirokazu, Shibayama Hirohiko, Sugahara Hiroyuki, Takai Emi, Zhang Xian, Machii Takashi, Kanakura Yuzuru
Abstract excerpt
The c-kit receptor tyrosine kinase (KIT) is constitutively activated by 2 types of naturally occurring mutations, the Val559-->Gly (G559) mutation in the juxtamembrane domain and the Asp814-->Val (V814) mutation in the catalytic domain. We evaluated the effects of the tyrosine kinase inhibitors STI571 and AG1296 on BaF3 cells expressing wild-type KIT (KIT(WT)) or activating mutants of KIT (KIT(G559) and...
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