| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 2139548 | Leukemia Research | 2008 | 4 Pages |
Abstract
We compared the growth-inhibitory effects and inhibition profile of the SRC family kinases (SFKs) of imatinib, dasatinib, nilotinib and INNO-406. Dasatinib exhibited the strongest potency against BCR–ABL with little selectivity over SFKs. Nilotinib exhibited a weaker affinity than the other inhibitors, but was highly specific for ABL and may be useful for the treatment of P-glycoprotein overexpressing leukemic cells. INNO-406 had an intermediate affinity for BCR–ABL between that of dasatinib and nilotinib, and inhibited only SFKs LCK and LYN among SFKs. Both nilotinib and INNO-406 were potent inhibitors of the dasatinib-resistant T315A, F317L and F317V BCR–ABL mutations.
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Authors
Yasuyuki Deguchi, Shinya Kimura, Eishi Ashihara, Tomoko Niwa, Keiko Hodohara, Yoshihide Fujiyama, Taira Maekawa,