Institute of Molecular Biology and Pathology (IBPM), National Research Council (CNR) of Italy, Rome, Italy.
Laboratory of Muscle Stem Cells and Gene Regulation, National Institute of Arthritis and Musculoskeletal and Skin Diseases (NIAMS), National Institutes of Health (NIH), Bethesda, MD, USA.
Trends Mol Med. 2024 Mar;30(3):278-294. doi: 10.1016/j.molmed.2024.01.007. Epub 2024 Feb 26.
Earlier evidence that targeting the balance between histone acetyltransferases (HATs) and deacetylases (HDACs), through exposure to HDAC inhibitors (HDACis), could enhance skeletal myogenesis, prompted interest in using HDACis to promote muscle regeneration. Further identification of constitutive HDAC activation in dystrophin-deficient muscles, caused by dysregulated nitric oxide (NO) signaling, provided the rationale for HDACi-based therapeutic interventions for Duchenne muscular dystrophy (DMD). In this review, we describe the molecular, preclinical, and clinical evidence supporting the efficacy of HDACis in countering disease progression by targeting pathogenic networks of gene expression in multiple muscle-resident cell types of patients with DMD. Given that givinostat is paving the way for HDACi-based interventions in DMD, next-generation HDACis with optimized therapeutic profiles and efficacy could be also explored for synergistic combinations with other therapeutic strategies.
早期有证据表明,通过暴露于组蛋白乙酰转移酶(HATs)和去乙酰化酶(HDACs)的平衡,靶向 HDAC 抑制剂(HDACis)可以增强骨骼肌生成,这引发了人们对使用 HDACis 促进肌肉再生的兴趣。进一步确定了肌营养不良蛋白缺乏的肌肉中存在组成性 HDAC 激活,这是由于一氧化氮(NO)信号的失调引起的,为基于 HDACi 的治疗干预杜氏肌营养不良症(DMD)提供了依据。在这篇综述中,我们描述了分子、临床前和临床证据,支持 HDACis 通过靶向 DMD 患者多种肌肉驻留细胞类型的致病基因表达网络,来对抗疾病进展的疗效。鉴于 givinostat 为 DMD 的基于 HDACi 的干预铺平了道路,因此可以探索具有优化治疗谱和疗效的下一代 HDACis,以与其他治疗策略进行协同组合。