The Activity of the Novel Aurora Kinase B Inhibitor AZD1152 in Acute Myeloid Leukaemia Cells.
Blood(2005)
摘要
Background: Aurora kinases (A, B and C) play a critical role in regulating mitosis and cell division. Aurora kinase A is required for correct spindle assembly while aurora kinase B is involved in histone H3 phosphorylation, chromosome segregation, and cytokinesis. Emerging data suggest these proteins are implicated in the survival and proliferation of both haematologic and solid malignancies, and therefore represent novel therapeutic targets. Several aurora kinase inhibitors have been described, mainly inhibiting both A and B kinases, although inhibition of aurora kinase B is more closely associated with the effects seen with these compounds. We have therefore investigated the activity of AZD1152, a novel, specific inhibitor of aurora kinase activity, with selectivity for aurora B.
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