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The role of Pin1 in the development and treatment of cancer

机译:Pin1在癌症发展和治疗中的作用

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摘要

Protein phosphorylation and post-phosphorylation events regulate many cellular signaling pathways. Peptidyl-prolyl isomerase (Pin1) is the only peptidyl-prolyl cis/trans isomerase that interacts with numerous oncogenic or tumor suppressive phosphorylated proteins, causes conformational changes in target proteins, and eventually regulates the activities of such proteins. These alterations in activity play a pivotal role in tumorigenesis. Since Pin1 is overexpressed and/or activated in various types of cancers, and the dysregulation of proline-directed phosphorylation contributes to tumorigenesis, Pin1 represents an attractive target for cancer therapy. This review will describe the role of Pin1 in cancer and the current status of Pin1 inhibitor development.
机译:蛋白质磷酸化和磷酸化后的事件调节许多细胞信号转导途径。肽基脯氨酰异构酶(Pin1)是唯一的肽基脯氨酰顺/反异构酶,可与多种致癌或肿瘤抑制性磷酸化蛋白相互作用,引起靶蛋白的构象变化,并最终调节此类蛋白的活性。这些活性改变在肿瘤发生中起关键作用。由于Pin1在各种类型的癌症中过表达和/或激活,并且脯氨酸指导的磷酸化失调促进了肿瘤的发生,因此Pin1代表了一种有吸引力的癌症治疗靶标。这篇综述将描述Pin1在癌症中的作用以及Pin1抑制剂发展的当前状态。

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