G9a an Epigenetic Therapeutic Strategy for Neurodegenerative Conditions: From Target Discovery to Clinical Trials

IF 10.9 1区医学 Q1 CHEMISTRY, MEDICINAL

Medicinal Research Reviews Pub Date : 2025-01-06 DOI:10.1002/med.22096

Aina Bellver-Sanchis, Marta Ribalta-Vilella, Alba Irisarri, Pinky Gehlot, Bhanwar Singh Choudhary, Abhisek Jana, Vivek Kumar Vyas, Deb Ranjan Banerjee, Mercè Pallàs, Ana Guerrero, Christian Griñán-Ferré

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引用次数: 0

Abstract

This review provides a comprehensive overview of the role of G9a/EHMT2, focusing on its structure and exploring the impact of its pharmacological and/or gene inhibition in various neurological diseases. In addition, we delve into the advancements in the design and synthesis of G9a/EHMT2 inhibitors, which hold promise not only as a treatment for neurodegeneration diseases but also for other conditions, such as cancer and malaria. Besides, we presented the discovery of dual therapeutic approaches based on G9a inhibition and different epigenetic enzymes like histone deacetylases, DNA methyltransferases, and other lysine methyltransferases. Hence, findings offer valuable insights into developing novel and promising therapeutic strategies targeting G9a/EHMT2 for managing these neurological conditions.

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神经退行性疾病的表观遗传治疗策略：从靶点发现到临床试验

本文综述了G9a/EHMT2的作用，重点介绍了其结构，并探讨了其在各种神经系统疾病中的药理和/或基因抑制作用。此外，我们还深入研究了G9a/EHMT2抑制剂的设计和合成方面的进展，这些抑制剂不仅有望治疗神经退行性疾病，还有望治疗其他疾病，如癌症和疟疾。此外，我们还发现了基于G9a抑制和不同表观遗传酶（如组蛋白去乙酰化酶、DNA甲基转移酶和其他赖氨酸甲基转移酶）的双重治疗方法。因此，研究结果为开发针对G9a/EHMT2的新颖且有前景的治疗策略来管理这些神经系统疾病提供了有价值的见解。

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

Medicinal Research Reviews 医学-药学

CiteScore

29.30

自引率

0.00%

发文量

审稿时长

2 months

期刊介绍： Medicinal Research Reviews is dedicated to publishing timely and critical reviews, as well as opinion-based articles, covering a broad spectrum of topics related to medicinal research. These contributions are authored by individuals who have made significant advancements in the field. Encompassing a wide range of subjects, suitable topics include, but are not limited to, the underlying pathophysiology of crucial diseases and disease vectors, therapeutic approaches for diverse medical conditions, properties of molecular targets for therapeutic agents, innovative methodologies facilitating therapy discovery, genomics and proteomics, structure-activity correlations of drug series, development of new imaging and diagnostic tools, drug metabolism, drug delivery, and comprehensive examinations of the chemical, pharmacological, pharmacokinetic, pharmacodynamic, and clinical characteristics of significant drugs.