Center for Human Genetics, KULeuven, Belgium.
Anticancer Agents Med Chem. 2011 Jan;11(1):38-46. doi: 10.2174/187152011794941172.
The kinase oncogenes are well-characterized drivers of cancer development, and several targeted therapies focused on both specific and selectively nonselective kinase inhibitors have now been approved for clinical use. In contrast, much less is known about the role of protein phosphatases, although modulation of their activities might form the foundation for an effective anti-cancer approach. The serine-threonine protein phosphatase 2A (PP2A) is implicated in the regulation of numerous signaling pathways and may function as a tumor suppressor. Recently pharmacological modulation of PP2A activity has been showed to have a potent anti-tumor activity in both in vitro and in vivo cancer models. These studies implicate PP2A as a promising therapeutic target for the treatment of cancer.
激酶癌基因是癌症发展的特征驱动因子,目前已有几种针对特定和选择性非选择性激酶抑制剂的靶向治疗药物获得临床批准。相比之下,人们对蛋白磷酸酶的作用知之甚少,尽管调节它们的活性可能为有效的抗癌方法奠定基础。丝氨酸-苏氨酸蛋白磷酸酶 2A(PP2A)参与了许多信号通路的调节,可能作为肿瘤抑制因子发挥作用。最近的研究表明,药理学调节 PP2A 的活性在体外和体内的癌症模型中均具有很强的抗肿瘤活性。这些研究表明 PP2A 是治疗癌症的一个有前途的治疗靶点。