Department of Pharmacology, University of Nevada, Reno School of Medicine, , Reno, NV, USA.
Division of Pre-clinical Innovation, NIH Center for Advancing Translational Sciences, Rockville, MD, USA.
Hum Mol Genet. 2019 Jul 1;28(13):2120-2132. doi: 10.1093/hmg/ddz044.
Duchenne muscular dystrophy (DMD) is a lethal, muscle degenerative disease causing premature death of affected children. DMD is characterized by mutations in the dystrophin gene that result in a loss of the dystrophin protein. Loss of dystrophin causes an associated reduction in proteins of the dystrophin glycoprotein complex, leading to contraction-induced sarcolemmal weakening, muscle tearing, fibrotic infiltration and rounds of degeneration and failed regeneration affecting satellite cell populations. The α7β1 integrin has been implicated in increasing myogenic capacity of satellite cells, therefore restoring muscle viability, increasing muscle force and preserving muscle function in dystrophic mouse models. In this study, we show that a Food and Drug Administration (FDA)-approved small molecule, Sunitinib, is a potent α7 integrin enhancer capable of promoting myogenic regeneration by stimulating satellite cell activation and increasing myofiber fusion. Sunitinib exerts its regenerative effects via transient inhibition of SHP-2 and subsequent activation of the STAT3 pathway. Treatment of mdx mice with Sunitinib demonstrated decreased membrane leakiness and damage owing to myofiber regeneration and enhanced support at the extracellular matrix. The decreased myofiber damage translated into a significant increase in muscle force production. This study identifies an already FDA-approved compound, Sunitinib, as a possible DMD therapeutic with the potential to treat other muscular dystrophies in which there is defective muscle repair.
杜氏肌营养不良症(DMD)是一种致命的肌肉退行性疾病,可导致受影响儿童过早死亡。DMD 的特征是肌营养不良蛋白基因突变,导致肌营养不良蛋白的缺失。肌营养不良蛋白的缺失导致肌营养不良糖蛋白复合物的相关蛋白减少,导致收缩诱导的肌膜弱化、肌肉撕裂、纤维浸润和一轮退化以及卫星细胞群的再生失败。α7β1 整联蛋白被认为可以增加卫星细胞的成肌能力,从而恢复肌肉活力,增加肌肉力量并在 DMD 小鼠模型中维持肌肉功能。在这项研究中,我们表明,一种已获得美国食品和药物管理局(FDA)批准的小分子药物舒尼替尼是一种有效的α7 整联蛋白增强剂,能够通过刺激卫星细胞激活和增加肌纤维融合来促进成肌再生。舒尼替尼通过短暂抑制 SHP-2 和随后激活 STAT3 通路发挥其再生作用。舒尼替尼治疗 mdx 小鼠可减少由于肌纤维再生和细胞外基质支持增强而导致的膜通透性和损伤。肌纤维损伤的减少转化为肌肉力量产生的显著增加。这项研究确定了一种已经获得 FDA 批准的化合物,舒尼替尼,作为一种可能的 DMD 治疗药物,具有治疗其他肌肉疾病的潜力,这些疾病存在肌肉修复缺陷。