将OP449归入PP2A激活药物家族。
SETting OP449 into the PP2A-activating drug family.
作者信息
Neviani Paolo, Perrotti Danilo
机构信息
Authors' Affiliations: The Ohio State University Comprehensive Cancer Center, Columbus, Ohio; and Department of Medicine, The Greenebaum Cancer Center, University of Maryland School of Medicine, Baltimore, Maryland.
出版信息
Clin Cancer Res. 2014 Apr 15;20(8):2026-8. doi: 10.1158/1078-0432.CCR-14-0166. Epub 2014 Mar 14.
Abstract
The protein phosphatase 2A (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 nontoxic PP2A-activating drugs (PAD), OP449 inhibits SET and impairs leukemogenesis. This further supports the immediate use of PADs in patients with leukemia.
摘要
蛋白磷酸酶2A（PP2A）肿瘤抑制因子在不同白血病中通过其内源性抑制剂（如SET）的活性而失活，这些抑制剂受到致癌酪氨酸激酶的异常调控。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。这进一步支持了在白血病患者中立即使用PAD。
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本文引用的文献
1
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2
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J Clin Invest. 2013 Oct;123(10):4144-57. doi: 10.1172/JCI68951. Epub 2013 Sep 3.
3
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Blood. 2013 Sep 12;122(11):1923-34. doi: 10.1182/blood-2013-03-492181. Epub 2013 Aug 7.
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8
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J Clin Invest. 2007 Sep;117(9):2408-21. doi: 10.1172/JCI31095.
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