SETting OP449 into the PP2A-activating drug family.
SETting OP449 into the PP2A-activating drug family.
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DOI：
10.1158/1078-0432.ccr-14-0166
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发表时间：
2014-04-15
期刊：
影响因子：
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通讯作者：
Perrotti D
中科院分区：
文献类型：
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作者：
Neviani P;Perrotti D
PP2A肿瘤抑制因子在不同的白血病中通过其内源性抑制因子（例如SET）的活性而失活，所述内源性抑制因子由致癌酪氨酸激酶异常调节。与其他有效且无毒的PP2A激活药物（PAD）一样，OP449抑制SET并损害白血病发生。这进一步支持在白血病患者中立即使用PAD。
The PP2A tumor suppressor is inactivated in different leukemias through the activity of its endogenous inhibitors (e.g. SET), which are aberrantly regulated by oncogenic tyrosine kinases. Like other effective and non-toxic PP2A-activating-drugs (PADs), OP449 inhibits SET and impairs leukemogenesis. This, further supports the immediate use of PADs in leukemia patients.