All roads lead to PP2A: exploiting the therapeutic potential of this phosphatase.
All roads lead to PP2A: exploiting the therapeutic potential of this phosphatase.
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DOI：
10.1111/febs.13573
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发表时间：
2016-03
期刊：
影响因子：
--
通讯作者：
Narla G
中科院分区：
文献类型：
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作者：
Sangodkar J;Farrington CC;McClinch K;Galsky MD;Kastrinsky DB;Narla G
蛋白磷酸酶2A是一种丝氨酸/苏氨酸磷酸酶，参与许多细胞过程的调控。作为一种已被确认的肿瘤抑制蛋白，PP2A在许多癌症中发生基因改变或功能失活，这凸显了对其进行治疗性激活的需求。在这篇综述中，我们将讨论有关PP2A的近期文献：其结构的阐明以及其亚基的功能，以及导致其在癌症中失调的分子损伤和翻译后修饰的鉴定。最后一部分将讨论调节PP2A的蛋白质和小分子，以及如何利用它们来靶向失调形式的PP2A以治疗癌症和其他疾病。
Protein phosphatase 2A is a serine/threonine phosphatase involved in the regulation of many cellular processes. A confirmed tumor suppressor protein, PP2A is genetically altered or functionally inactivated in many cancers highlighting a need for its therapeutic reactivation. In this review we will discuss recent literature on PP2A: the elucidation of its structure and the functions of its subunits, and the identification of molecular lesions and post-translational modifications leading to its dysregulation in cancer. A final section will discuss the proteins and small molecules that modulate PP2A and how these might be used to target dysregulated forms of PP2A to treat cancers and other diseases.