组蛋白
表观遗传学
乙酰化
HDAC11型
组蛋白脱乙酰基酶
生物
癌症表观遗传学
计算生物学
细胞生物学
化学
癌症研究
DNA
基因
遗传学
组蛋白甲基转移酶
作者
Diaaeldin I. Abdallah,Elvin D. de Araujo,Naman H. Patel,Lina S. Hasan,Richard Moriggl,Oliver H. Krämer,Patrick T. Gunning
标识
DOI:10.37349/etat.2023.00166
摘要
Histone deacetylases (HDACs) are a class of zinc (Zn)-dependent metalloenzymes that are responsible for epigenetic modifications. HDACs are largely associated with histone proteins that regulate gene expression at the DNA level. This tight regulation is controlled by acetylation [via histone acetyl transferases (HATs)] and deacetylation (via HDACs) of histone and non-histone proteins that alter the coiling state of DNA, thus impacting gene expression as a downstream effect. For the last two decades, HDACs have been studied extensively and indicated in a range of diseases where HDAC dysregulation has been strongly correlated with disease emergence and progression—most prominently, cancer, neurodegenerative diseases, HIV, and inflammatory diseases. The involvement of HDACs as regulators in these biochemical pathways established them as an attractive therapeutic target. This review summarizes the drug development efforts exerted to create HDAC inhibitors (HDACis), specifically class I HDACs, with a focus on the medicinal chemistry, structural design, and pharmacology aspects of these inhibitors.
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