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Histone deacetylase inhibitors: A chemical genetics approach to understanding cellular functions

机译:组蛋白脱乙酰基酶抑制剂:了解细胞功能的化学遗传学方法

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摘要

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.
机译:人类中有11种锌依赖性组蛋白脱乙酰基酶(HDAC),它们具有组蛋白和许多非组蛋白底物。这些酶的底物包括在调节基因表达,细胞增殖,细胞迁移,细胞死亡,免疫途径和血管生成中起作用的蛋白质。已经开发出HDACs(HDACi)抑制剂,这些抑制剂可改变这些蛋白质的结构和功能,从而引起分子和细胞变化,从而诱导转化的细胞死亡。 HDACi正在开发为抗癌药物,对许多非肿瘤性疾病具有治疗潜力。

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