Targets and effectors of the cellular response to aurora kinase inhibitor mk-0457 (vx-680) in imatinib sensitive and resistant chronic myelogenous leukemia.

Posted by rob on November 1, 2009 under Uncategorized | Comments are off for this article

TARGETS AND EFFECTORS OF THE CELLULAR RESPONSE TO AURORA KINASE INHIBITOR MK-0457 (VX-680) IN IMATINIB SENSITIVE AND RESISTANT CHRONIC MYELOGENOUS LEUKEMIA.
Biochem Pharmacol. 2009 Oct 26;
Authors: Donato NJ, Feng D, Sun H, Giannola D, Peterson LF, Talpaz M
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 – 100nM and 2 – 10muM MK-0457, respectively, but expression of T315I-BCR-ABL and overexpression of Lyn kinase reduced MK-0457 sensitivity. Aurora kinase inhibition was associated with cell cy…
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