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组蛋白去乙酰化酶抑制剂作为一种针对非小细胞肺癌的新型靶向治疗方法:我们目前的进展以及未来的展望如何?

Histone Deacetylase Inhibitors as a Novel Targeted Therapy Against Non-small Cell Lung Cancer: Where Are We Now and What Should We Expect?

作者信息

Damaskos Christos, Tomos Ioannis, Garmpis Nikolaos, Karakatsani Anna, Dimitroulis Dimitrios, Garmpi Anna, Spartalis Eleftherios, Kampolis Christos F, Tsagkari Eleni, Loukeri Angeliki A, Margonis Georgios-Antonios, Spartalis Michael, Andreatos Nikolaos, Schizas Dimitrios, Kokkineli Stefania, Antoniou Efstathios A, Nonni Afroditi, Tsourouflis Gerasimos, Markatos Konstantinos, Kontzoglou Konstantinos, Kostakis Alkiviadis, Tomos Periklis

机构信息

Second Department of Propedeutic Surgery, Laiko General Hospital, Medical School, National and Kapodistrian University of Athens, Athens, Greece

N.S. Christeas Laboratory of Experimental Surgery and Surgical Research, Medical School, National and Kapodistrian University of Athens, Athens, Greece.

出版信息

Anticancer Res. 2018 Jan;38(1):37-43. doi: 10.21873/anticanres.12189.

Abstract

Non-small cell lung cancer constitutes the most common type of lung cancer, accounting for 85-90% of lung cancer, and is a leading cause of cancer-related death. Despite the progress during the past years, poor prognosis remains a challenge and requires further research and development of novel antitumor treatment. Recently, the role of histone deacetylases in gene expression has emerged showing their regulation of the acetylation of histone proteins and other non-histone protein targets and their role in chromatin organization, while their inhibitors, the histone deacetylase inhibitors, have been proposed to have a potential therapeutic role in diverse malignancies, including non-small cell lung cancer. This review article focuses on the role of histone deacetylase inhibitors in the treatment of non-small cell lung cancer and the major molecular mechanisms underlying their antitumor activity recognized so far.

摘要

非小细胞肺癌是最常见的肺癌类型,占肺癌的85-90%,是癌症相关死亡的主要原因。尽管在过去几年中取得了进展,但预后不良仍然是一个挑战,需要进一步研究和开发新的抗肿瘤治疗方法。最近,组蛋白去乙酰化酶在基因表达中的作用逐渐显现,表明它们对组蛋白和其他非组蛋白靶点的乙酰化具有调节作用,以及在染色质组织中的作用,而其抑制剂,即组蛋白去乙酰化酶抑制剂,已被提出在包括非小细胞肺癌在内的多种恶性肿瘤中具有潜在的治疗作用。本文综述聚焦于组蛋白去乙酰化酶抑制剂在非小细胞肺癌治疗中的作用以及目前所认识到的其抗肿瘤活性的主要分子机制。

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