Imatinib has the potential to exert its antileukemia effects by down-regulating hERG1 K+ channels in chronic myelogenous leukemia

Posted by rob on January 9, 2012 under Uncategorized | Comments are off for this article

Abstract  Imatinib is a powerful protein tyrosine kinase (PTK) inhibitor that specifically targets BCR-ABL, KIT, and PDGFR kinases,
has become the current first-line therapy for all newly diagnosed chronic myeloid leukemia (CML). Beside PTKs, PTK inhibitors
alter the activity of a large number of voltage-dependent ion channels. hERG1 K+ channels are highly expressed in leukemia cells and appear of exceptional importance in favoring leukemogenesis. The present
study explored a possible regulatory effect of imatinib upon hERG1 K+ channels as a means to uncover new molecular events involved in the antileukemic activity of this PTK inhibitor in CML. The
results demonstrated that hERG1 was highly detected in K562 cells and primary CML cells, and down-regulated by imatinib at
mRNA…
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