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中华针灸电子杂志 ›› 2014, Vol. 03 ›› Issue (03) : 120 -123. doi: 10.3877/cma.j.issn.2095-3240.2014.03.005

综述

端锚聚合酶1 在肿瘤治疗中研究进展
李翀1,(), 郑旭1   
  1. 1.300193 天津中医药大学第一附属医院病理科
  • 收稿日期:2014-01-22 出版日期:2014-06-15
  • 通信作者: 李翀

Progress of telomerase 1 in cancer treatment

Chong Li1,(), Xu Zheng1   

  1. 1.Department of Pathology,First Teaching Hospital of Tianjin University of Traditional Chinese Medicine,Tianjin 300193,China
  • Received:2014-01-22 Published:2014-06-15
  • Corresponding author: Chong Li
引用本文:

李翀, 郑旭. 端锚聚合酶1 在肿瘤治疗中研究进展[J/OL]. 中华针灸电子杂志, 2014, 03(03): 120-123.

Chong Li, Xu Zheng. Progress of telomerase 1 in cancer treatment[J/OL]. Chinese Journal of Acupuncture and Moxibustion(Electronic Edition), 2014, 03(03): 120-123.

端锚聚合酶1(TNKS 1)可通过对端粒结合蛋白1 的糖基化修饰调节,使端粒维持在一定长度,导致肿瘤的发生。 在许多恶性肿瘤中,TNKS 1 蛋白呈高水平表达。 端锚聚合酶抑制剂具有抗肿瘤活性,小分子端锚聚合酶抑制剂可通过稳定轴蛋白表达,诱导β-连环蛋白降解,对抗Wnt 信号转导途径,从而抑制肿瘤生长。Wnt 信号系统中的许多生物学进程和致病过程都受TNKS 1 和TNKS 1 抑制剂的调控。此外,联合应用TNKS 1 抑制剂与其他抑制剂,可使肿瘤细胞发生坏死和凋亡的时间明显缩短。TNKS 1 及其小分子抑制剂在维持端粒动态平衡和Wnt/β-catenin 信号转导中的作用机制日益明确,成为肿瘤靶向治疗的潜在研究药物。 重点讨论TNKS 1 的生物学特性,新型TNKS 1 的特异性抑制剂及其在肿瘤临床治疗中的应用现状。

Tankyrase 1(TNKS 1)can maintain the telomere length by modifying telomere-binding protein glycosylation, leading tumorigenesis. In many cancers, TNKS 1 protein was expressed at high levels. Tankyrase inhibitors have anti-tumor activity. The small molecule tyrosine kinase inhibitors can induce the β-catenin degradation and antagonizing Wnt signaling by stabilizing protein expression,restraining tumor growth. Many biological processes and the pathogenic process of Wnt signal system are regulated by TNKS 1 and TNKS 1 inhibitors. In addition, the combined use of TNKS 1 inhibitors with other inhibitors can shorten the time of necrosis and apoptosis of tumor cells. Recent research offers insights into the role of TNKS 1 and TNKS 1 inhibitors in maintaining telomere dynamic balance and regulating the Wnt/β-catenin pathway, which may hold promise for cancer therapy. This article reviews the bionomics of TNKS 1 and new type specific inhibitor of TNKS 1 and discusses its current application in clinic cancer therapy.

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