Yoon Somy, Eom Gwang Hyeon
Department of Pharmacology, Chonnam National University Medical School, Gwangju, Korea.
Chonnam Med J. 2016 Jan;52(1):1-11. doi: 10.4068/cmj.2016.52.1.1. Epub 2016 Jan 19.
Histone deacetylases (HDACs) are epigenetic regulators that regulate the histone tail, chromatin conformation, protein-DNA interaction, and even transcription. HDACs are also post-transcriptional modifiers that regulate the protein acetylation implicated in several pathophysiologic states. HDAC inhibitors have been highlighted as a novel category of anti-cancer drugs. To date, four HDAC inhibitors, Vorinostat, Romidepsin, Panobinostat, and Belinostat, have been approved by the United States Food and Drug Administration. Principally, these HDAC inhibitors are used for hematologic cancers in clinic with less severe side effects. Clinical trials are continuously expanding to address other types of cancer and also nonmalignant diseases. HDAC inhibition also results in beneficial outcomes in various types of neurodegenerative diseases, inflammation disorders, and cardiovascular diseases. In this review, we will briefly discuss 1) the roles of HDACs in the acquisition of a cancer's phenotype and the general outcome of the HDAC inhibitors in cancer, 2) the functional relevance of HDACs in cardiovascular diseases and the possible therapeutic implications of HDAC inhibitors in cardiovascular disease.
组蛋白去乙酰化酶（HDACs）是表观遗传调节剂，可调节组蛋白尾巴、染色质构象、蛋白质 - DNA相互作用，甚至转录。HDACs也是转录后修饰因子，可调节与多种病理生理状态相关的蛋白质乙酰化。HDAC抑制剂已成为一类新型抗癌药物。迄今为止，伏立诺他、罗米地辛、帕比司他和贝利司他这四种HDAC抑制剂已获得美国食品药品监督管理局的批准。在临床上，这些HDAC抑制剂主要用于血液系统癌症，副作用相对较轻。临床试验正在不断扩展，以针对其他类型的癌症以及非恶性疾病。HDAC抑制在各种类型的神经退行性疾病、炎症性疾病和心血管疾病中也产生了有益的结果。在本综述中，我们将简要讨论：1）HDACs在癌症表型获得中的作用以及HDAC抑制剂在癌症中的总体疗效；2）HDACs在心血管疾病中的功能相关性以及HDAC抑制剂在心血管疾病中的可能治疗意义。
