表观遗传小分子筛选鉴定一种新的HDACi化合物改善杜氏肌营养不良症。

IF 6.1 2区 医学 Q1 MEDICINE, RESEARCH & EXPERIMENTAL
Molecular Therapy. Nucleic Acids Pub Date : 2025-08-13 eCollection Date: 2025-09-09 DOI:10.1016/j.omtn.2025.102683
Ke'ale W Louie, Eva H Hasegawa, Gist H Farr, Amanda C Ignacz, Alison Paguio, Alyssa Maenza, Alison G Paquette, Clarissa A Henry, Lisa Maves
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引用次数: 0

摘要

杜氏肌营养不良症(DMD)是最常见的遗传性肌肉疾病。目前很少有有效的治疗方法来治疗这种疾病,尽管许多方法正在寻求。某些组蛋白去乙酰化酶抑制剂(HDACi)已被证明可以改善小鼠和斑马鱼模型中的DMD表型,并且HDACi givinostat最近获得了FDA对DMD的批准。我们的目标是确定对DMD有益的其他hdac或其他类型的表观遗传小分子。利用已建立的DMD动物模型,斑马鱼DMD突变株sapje,我们筛选了800多个表观遗传小分子文库。我们的筛选确定了一种新的HDACi SR-4370,它可以改善dmd突变斑马鱼的骨骼肌退化,以及其他先前被证明可以改善dmd斑马鱼的HDACi。我们发现单次早期治疗HDACi可以改善dmd斑马鱼的肌肉表型并延长寿命。此外,我们发现改善dmd肌肉的HDACi处理也导致斑马鱼幼虫组蛋白乙酰化增加。我们的研究结果进一步证明,HDACi是治疗DMD的有希望的候选药物。本研究也为dmd斑马鱼小分子筛选的有效性提供了进一步的支持。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Epigenetic small molecule screening identifies a new HDACi compound for ameliorating Duchenne muscular dystrophy.

Duchenne muscular dystrophy (DMD) is the most common inherited muscle disease. There are currently few effective therapies to treat the disease, although many approaches are being pursued. Certain histone deacetylase inhibitors (HDACi) have been shown to ameliorate DMD phenotypes in mouse and zebrafish models, and the HDACi givinostat has recently gained FDA approval for DMD. Our goal was to identify additional HDACi, or other classes of epigenetic small molecules, that are beneficial for DMD. Using an established animal model for DMD, the zebrafish dmd mutant strain sapje, we screened a library of over 800 epigenetic small molecules. Our screening identified a new HDACi, SR-4370, that ameliorated dmd mutant zebrafish skeletal muscle degeneration, as well as additional HDACi that have previously been shown to improve dmd zebrafish. We find that a single early treatment of HDACi can ameliorate the muscle phenotype and increase lifespan in dmd zebrafish. Furthermore, we find that HDACi treatments that improve dmd muscle also cause increased histone acetylation in zebrafish larvae. Our results add to the growing evidence that HDACi are promising candidates for treating DMD. Our study also provides further support for the effectiveness of small molecule screening in dmd zebrafish.

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来源期刊
Molecular Therapy. Nucleic Acids
Molecular Therapy. Nucleic Acids MEDICINE, RESEARCH & EXPERIMENTAL-
CiteScore
15.40
自引率
1.10%
发文量
336
审稿时长
20 weeks
期刊介绍: Molecular Therapy Nucleic Acids is an international, open-access journal that publishes high-quality research in nucleic-acid-based therapeutics to treat and correct genetic and acquired diseases. It is the official journal of the American Society of Gene & Cell Therapy and is built upon the success of Molecular Therapy. The journal focuses on gene- and oligonucleotide-based therapies and publishes peer-reviewed research, reviews, and commentaries. Its impact factor for 2022 is 8.8. The subject areas covered include the development of therapeutics based on nucleic acids and their derivatives, vector development for RNA-based therapeutics delivery, utilization of gene-modifying agents like Zn finger nucleases and triplex-forming oligonucleotides, pre-clinical target validation, safety and efficacy studies, and clinical trials.
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