Article
Imatinib binding and cKIT inhibition is abrogated by the cKIT kinase domain I missense mutation Val654Ala.
Molecular cancer therapeutics - 1 Dec 2005
McLean Sean R, Gana-Weisz Mali, Hartzoulakis Basil, Frow Richard, Whelan Jeremy, Selwood David, Boshoff Chris
Abstract excerpt
Several activating mutations in the cKIT receptor tyrosine kinase are associated with the development and progression of gastrointestinal stromal tumors (GIST). Treatment of GIST with the tyrosine kinase inhibitor imatinib (Gleevec, STI571; Novartis, Basel, Switzerland) increases patient survival. However, many patients develop resistance to imatinib following initial responses. We sequenced cKIT exons from two...
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