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蛋白质磷酸化在细胞信号转导中的关键作用及其作为靶向治疗的应用(综述)。

The crucial role of protein phosphorylation in cell signaling and its use as targeted therapy (Review).

机构信息

Department of Clinical and Experimental Medicine, Foggia University, I-71122 Foggia, Italy.

出版信息

Int J Mol Med. 2017 Aug;40(2):271-280. doi: 10.3892/ijmm.2017.3036. Epub 2017 Jun 22.

Abstract

Protein phosphorylation is an impo-rtant cellular regulatory mechanism as many enzymes and receptors are activated/deactivated by phosphorylation and dephosphorylation events, by means of kinases and phosph-atases. In particular, the protein kinases are responsible for cellular transduction signaling and their hyperactivity, malfunction or overexpression can be found in several diseases, mostly tumors. Therefore, it is evident that the use of kinase inhibitors can be valuable for the treatment of cancer. In this review, we discuss the mechanism of action of phosphorylation, with particular attention to the importance of phosphorylation under physiological and pathological conditions. We also discuss the possibility of using kinase inhibitors in the treatment of tumors.

摘要

蛋白质磷酸化是一种重要的细胞调节机制,因为许多酶和受体通过磷酸化和去磷酸化事件被激酶和磷酸酶激活/失活。特别是,蛋白激酶负责细胞转导信号,它们的过度活跃、功能障碍或过度表达可在多种疾病中发现,主要是肿瘤。因此,使用激酶抑制剂治疗癌症显然是有价值的。在这篇综述中,我们讨论了磷酸化的作用机制,特别关注了在生理和病理条件下磷酸化的重要性。我们还讨论了使用激酶抑制剂治疗肿瘤的可能性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd37/5500920/575cfc7f7a4b/IJMM-40-02-0271-g00.jpg

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