作者
AS Moore, J Blagg, S Linardopoulos, ADJ Pearson
发表日期
2010/4/1
来源
Leukemia
卷号
24
期号
4
页码范围
671-678
出版商
Nature Publishing Group
简介
Aurora kinases are a family of protein kinases that have a key role in multiple stages of mitosis. Over-expression of Aurora kinases, particularly Aurora A, has been demonstrated in a number of solid tumors and hematological malignancies. Not surprisingly, these serine/threonine kinases have become attractive small molecule targets for cancer therapeutics, with several inhibitors currently in early-phase clinical trials. A small number of compounds developed to date are highly selective for either Aurora A or Aurora B, while the majority inhibit both Aurora A and Aurora B; many of these compounds exhibit ‘off-target’inhibition of kinases such as ABL, JAK2 and FLT3. It is currently unclear whether the therapeutic activity of these compounds in leukemia is primarily due to selective Aurora or multi-kinase inhibition. The most promising application for Aurora kinase inhibitors to date appears to be in FLT3-mutated acute …
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