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Targeting DNA-PK in cancer.
Mutation Research/Fundamental and Molecular Mechanisms of Mutagenesis ( IF 2.3 ) Pub Date : 2020-02-25 , DOI: 10.1016/j.mrfmmm.2020.111692
Giovanna Damia 1
Affiliation  

DNA-dependent protein kinase (DNA-PK) is involved in many cellular pathways. It has a key role in the cellular response to DNA damage, in the repair of DNA double-strand break (DNA-DSBs) and as a consequence an important role in maintaining genomic integrity. In addition, DNA-PK has been shown to modulate transcription, to be involved in the development of the immune system and to protect telomeres. These pleotropic involvements and the fact that its expression is de-regulated in cancer have made DNA-PK an intriguing therapeutic target in cancer therapy, especially when combined with agents causing DNA-DSBs such as topoisomerase II inhibitors and ionizing radiation. Different small molecule inhibitors of DNA-PK have been recently synthesized and some are now being tested in clinical trials. This review discusses what is known about DNA-PK, its role in tumor biology, DNA repair and cancer therapy and critically discusses its inhibition as a potential therapeutic approach.

中文翻译:

在癌症中靶向DNA-PK。

DNA依赖性蛋白激酶(DNA-PK)参与许多细胞途径。它在细胞对DNA损伤的反应,DNA双链断裂(DNA-DSB)的修复中起关键作用,因此在维持基因组完整性方面也起着重要作用。此外,DNA-PK已被证明可调节转录,参与免疫系统的发育并保护端粒。这些多效性的介入及其在癌症中表达失调的事实使DNA-PK成为癌症治疗中引人入胜的治疗靶标,尤其是当与引起DNA-DSB的药物(例如拓扑异构酶II抑制剂和电离辐射)组合使用时。最近已经合成了不同的DNA-PK小分子抑制剂,其中一些正在临床试验中进行测试。这篇评论讨论了有关DNA-PK的知识,
更新日期:2020-02-25
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