靶向组蛋白的翻译后修饰用于癌症治疗。

Targeting post-translational modifications of histones for cancer therapy.

作者信息

Hsu Y-C, Hsieh Y-H, Liao C-C, Chong L-W, Lee C-Y, Yu Y-L, Chou R-H

机构信息

Mackay Medical College Institute of Biomedical Sciences New Taipei City Taiwan.

Chung Shan Medical University Department of Biochemistry, School of Medicine Taichung Taiwan.

出版信息

Cell Mol Biol (Noisy-le-grand). 2015 Oct 30;61(6):69-84.

PMID:26518898

Abstract

Post-translational modifications (PTMs) on histones including acetylation, methylation, phosphorylation, citrullination, ubiquitination, ADP ribosylation, and sumoylation, play important roles in different biological events including chromatin dynamics, DNA replication, and transcriptional regulation. Aberrant histones PTMs leads to abnormal gene expression and uncontrolled cell proliferation, followed by development of cancers. Therefore, targeting the enzymes required for specific histone PTMs holds a lot of potential for cancer treatment. In this review article, we retrospect the latest studies in the regulations of acetylation, methylation, and phosphorylation of histones. We also summarize inhibitors/drugs that target these modifications for cancer treatment.

摘要

组蛋白上的翻译后修饰（PTMs），包括乙酰化、甲基化、磷酸化、瓜氨酸化、泛素化、ADP核糖基化和类泛素化，在不同的生物学事件中发挥重要作用，包括染色质动力学、DNA复制和转录调控。异常的组蛋白PTMs会导致基因表达异常和细胞增殖失控，进而引发癌症。因此，针对特定组蛋白PTMs所需的酶进行靶向治疗在癌症治疗方面具有很大潜力。在这篇综述文章中，我们回顾了组蛋白乙酰化、甲基化和磷酸化调控方面的最新研究。我们还总结了针对这些修饰用于癌症治疗的抑制剂/药物。