HDAC9 as a Privileged Target: Reviewing its Role in Different Diseases and Structure-activity Relationships (SARs) of its Inhibitors.

IF 3.3 3区医学 Q2 CHEMISTRY, MEDICINAL

Mini reviews in medicinal chemistry Pub Date : 2024-01-01 DOI:10.2174/0113895575267301230919165827

Totan Das, Samima Khatun, Tarun Jha, Shovanlal Gayen

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引用次数: 0

Abstract

HDAC9 is a histone deacetylase enzyme belonging to the class IIa of HDACs which catalyses histone deacetylation. HDAC9 inhibit cell proliferation by repairing DNA, arresting the cell cycle, inducing apoptosis, and altering genetic expression. HDAC9 plays a significant part in human physiological system and are involved in various type of diseases like cancer, diabetes, atherosclerosis and CVD, autoimmune response, inflammatory disease, osteoporosis and liver fibrosis. This review discusses the role of HDAC9 in different diseases and structure-activity relationships (SARs) of various hydroxamate and non-hydroxamate-based inhibitors. SAR of compounds containing several scaffolds have been discussed in detail. Moreover, structural requirements regarding the various components of HDAC9 inhibitor (cap group, linker and zinc-binding group) has been highlighted in this review. Though, HDAC9 is a promising target for the treatment of a number of diseases including cancer, a very few research are available. Thus, this review may provide useful information for designing novel HDAC9 inhibitors to fight against different diseases in the future.

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HDAC9作为特权靶点：回顾其在不同疾病中的作用及其抑制剂的结构-活性关系。

HDAC9是一种组蛋白去乙酰化酶，属于HDAC的IIa类，催化组蛋白脱乙酰化。HDAC9通过修复DNA、阻断细胞周期、诱导细胞凋亡和改变基因表达来抑制细胞增殖。HDAC9在人体生理系统中起着重要作用，并参与多种疾病，如癌症、糖尿病、动脉粥样硬化和心血管疾病、自身免疫反应、炎症性疾病、骨质疏松症和肝纤维化。这篇综述讨论了HDAC9在不同疾病中的作用，以及各种基于羟肟和非羟肟的抑制剂的构效关系。已经详细讨论了含有几种支架的化合物的SAR。此外，关于HDAC9抑制剂的各种成分（帽基、连接基和锌结合基）的结构要求在本综述中得到了强调。尽管HDAC9是治疗包括癌症在内的多种疾病的有前景的靶点，但很少有研究可用。因此，这篇综述可能为设计新的HDAC9抑制剂以对抗未来的不同疾病提供有用的信息。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Mini reviews in medicinal chemistry 医学-医药化学

CiteScore

7.80

自引率

0.00%

发文量

231

审稿时长

6 months

期刊介绍： The aim of Mini-Reviews in Medicinal Chemistry is to publish short reviews on the important recent developments in medicinal chemistry and allied disciplines. Mini-Reviews in Medicinal Chemistry covers all areas of medicinal chemistry including developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, drug targets, and natural product research and structure-activity relationship studies. Mini-Reviews in Medicinal Chemistry is an essential journal for every medicinal and pharmaceutical chemist who wishes to be kept informed and up-to-date with the latest and most important developments.