组蛋白去乙酰化酶抑制剂：一种用于理解细胞功能的化学遗传学方法。
Histone deacetylase inhibitors: a chemical genetics approach to understanding cellular functions.
作者信息
Marks Paul A
机构信息
Cell Biology and Genetics Program, Sloan-Kettering Institute for Cancer Research, Memorial Sloan-Kettering Cancer Center, New York, NY 10065, USA.
出版信息
Biochim Biophys Acta. 2010 Oct-Dec;1799(10-12):717-25. doi: 10.1016/j.bbagrm.2010.05.008. Epub 2010 Jun 8.
Abstract
There are eleven zinc dependent histone deacetylases (HDAC) in humans which have histones and many non-histone substrates. The substrates of these enzymes include proteins that have a role in regulation of gene expression, cell proliferation, cell migration, cell death, immune pathways and angiogenesis. Inhibitors of HDACs (HDACi) have been developed which alter the structure and function of these proteins, causing molecular and cellular changes that induce transformed cell death. The HDACi are being developed as anti-cancer drugs and have therapeutic potential for many non-oncologic diseases.
摘要
人类中有11种锌依赖性组蛋白脱乙酰酶（HDAC），它们作用于组蛋白以及许多非组蛋白底物。这些酶的底物包括在基因表达调控、细胞增殖、细胞迁移、细胞死亡、免疫途径和血管生成中发挥作用的蛋白质。HDAC抑制剂（HDACi）已被开发出来，它们会改变这些蛋白质的结构和功能，引起分子和细胞变化，从而诱导转化细胞死亡。HDACi正被开发用作抗癌药物，对许多非肿瘤性疾病也具有治疗潜力。
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