Biochemical Pharmacology volume 79, issue 5, P688-697 2010 DOI: 10.1016/j.bcp.2009.10.009 View full text
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Nicholas J. Donato, Dexing Fang, Hanshi Sun, Diane Giannola, Luke F. Peterson, Moshe Talpaz

Abstract: MK-0457 inhibits aurora, BCR-ABL and other kinases and may be clinically active in imatinib resistant leukemia. To define mediators of MK-0457 responsiveness, kinase inhibitory profiles were examined in multiple cell models of imatinib sensitive and resistant disease. Aurora and BCR-ABL kinase inhibition were consistently measured at 20-100 nM and 2-10 microM MK-0457, respectively, but expression of T315I-BCR-ABL and overexpression of Lyn kinase reduced MK-0457 sensitivity. Aurora kinase inhibition was associa…

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