Neurogenetics Branch, National Institute of Neurological Disorders and Stroke, National Institutes of Health, 35-2A1000, 35 Convent Dr., Bethesda, MD 20892, USA.
Prog Neurobiol. 2012 Dec;99(3):257-61. doi: 10.1016/j.pneurobio.2012.05.012. Epub 2012 Jun 2.
Spinal and bulbar muscular atrophy is unique among the polyglutamine diseases in that the toxicity of the mutant protein, the androgen receptor, is ligand-dependent. In cell culture and animal models the mutant androgen receptor causes protein aggregation and alterations in transcriptional regulation, axonal transport, and mitochondrial function. Various therapeutic approaches have shown efficacy in mouse models, including androgen reduction and agents that alter the processing and degradation of the mutant androgen receptor protein, such as HSP90 inhibitors, IGF-1, and ASC-J9. Clinical trials of androgen-reducing agents have shown indications of efficacy but not proof of clinically meaningful benefit to date. This trial experience has set the stage for future clinical studies of other agents that have been found to be beneficial in transgenic animal models.
脊髓延髓肌肉萎缩症在多聚谷氨酰胺疾病中是独特的,因为突变蛋白雄激素受体的毒性是配体依赖性的。在细胞培养和动物模型中,突变雄激素受体导致蛋白质聚集和转录调节、轴突运输和线粒体功能的改变。各种治疗方法在小鼠模型中显示出疗效,包括雄激素减少和改变突变雄激素受体蛋白的处理和降解的药物,如 HSP90 抑制剂、IGF-1 和 ASC-J9。雄激素减少剂的临床试验显示出疗效的迹象,但迄今为止还没有证明对临床有意义的益处。这一试验经验为其他已在转基因动物模型中发现有益的药物的未来临床研究奠定了基础。