| Literature DB >> 18191450 |
Yasuyuki Deguchi1, Shinya Kimura, Eishi Ashihara, Tomoko Niwa, Keiko Hodohara, Yoshihide Fujiyama, Taira Maekawa.
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.Entities:
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Year: 2008 PMID： 18191450 DOI： 10.1016/j.leukres.2007.11.008
Source DB: PubMed Journal: Leuk Res ISSN： 0145-2126 Impact factor: 3.156