靶向组蛋白去乙酰化酶:癌症之外的新兴应用

IF 6.5 2区 医学 Q1 PHARMACOLOGY & PHARMACY Drug Discovery Today Pub Date : 2024-07-10 DOI:10.1016/j.drudis.2024.104094
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引用次数: 0

摘要

组蛋白去乙酰化酶(HDACs)是一类特殊的水解酶,通过对细胞乙酰化的表观遗传控制,在染色质整合、细胞因子信号转导和基因表达等各种过程中发挥调节作用。HDAC 对细胞功能的广泛影响表明,HDAC 活性失调与人类疾病有关。虽然 HDAC 传统上是肿瘤学的靶点,但在过去十年中,除癌症外,多个治疗领域的抑制策略也有了显著的发展。本综述将重点介绍其中四个适应症(神经退行性疾病、代谢紊乱、心血管疾病和病毒感染)的研究进展,重点关注去乙酰化酶在疾病中的作用、小分子药物的发现以及临床进展。
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Targeting histone deacetylases: Emerging applications beyond cancer

Histone deacetylases (HDACs) are a special class of hydrolase enzymes, which through epigenetic control of cellular acetylation, play regulatory roles in various processes including chromatin packing, cytokine signaling, and gene expression. Widespread influence on cell function has implicated dysregulated HDAC activity in human disease. While traditionally an oncology target, in the past decade, there has been a notable rise in inhibition strategies within several therapeutic areas beyond cancer. This review highlights advances in four of these indications, neurodegenerative disease, metabolic disorders, cardiovascular disease, and viral infections, focusing on the role of deacetylases in disease, small molecule drug discovery, and clinical progress.

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来源期刊
Drug Discovery Today
Drug Discovery Today 医学-药学
CiteScore
14.80
自引率
2.70%
发文量
293
审稿时长
6 months
期刊介绍: Drug Discovery Today delivers informed and highly current reviews for the discovery community. The magazine addresses not only the rapid scientific developments in drug discovery associated technologies but also the management, commercial and regulatory issues that increasingly play a part in how R&D is planned, structured and executed. Features include comment by international experts, news and analysis of important developments, reviews of key scientific and strategic issues, overviews of recent progress in specific therapeutic areas and conference reports.
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