Neuronal Survival Unit, Wallenberg Neuroscience Center, Lund University, BMC A10, 221 84 Lund, Sweden.
Trends Pharmacol Sci. 2010 Nov;31(11):523-7. doi: 10.1016/j.tips.2010.08.005. Epub 2010 Sep 20.
Spinal and bulbar muscular atrophy is a hereditary motor neuron disease caused by trinucleotide repeat expansion in the androgen receptor gene. The disease mechanism probably involves a toxic gain of function in the mutant protein, because other mutations that cause a loss of androgen receptor function result in a different phenotype and the mutant protein is toxic in mouse models. In these models, the toxicity is ligand-dependent and is associated with protein aggregation, as well as altered transcriptional regulation, axonal transport and mitochondrial function. Various therapeutic approaches have shown efficacy in mouse models, including androgen reduction, heat shock protein 90 (HSP90) inhibition and insulin-like growth factor (IGF)-1 overexpression. Clinical trials of androgen-reducing agents have had mixed results, with indications of efficacy but no proof of clinically meaningful benefit to date. These clinical studies have established outcome measures for future trials of other agents that have been beneficial in animal studies.
脊髓延髓肌肉萎缩症是一种遗传性运动神经元疾病,由雄激素受体基因中的三核苷酸重复扩展引起。该疾病的机制可能涉及突变蛋白的毒性获得功能,因为导致雄激素受体功能丧失的其他突变会导致不同的表型,并且突变蛋白在小鼠模型中是有毒的。在这些模型中,毒性是配体依赖性的,与蛋白质聚集以及转录调节、轴突运输和线粒体功能的改变有关。各种治疗方法在小鼠模型中显示出疗效,包括雄激素减少、热休克蛋白 90(HSP90)抑制和胰岛素样生长因子(IGF)-1过表达。雄激素减少剂的临床试验结果喜忧参半,表明有疗效,但迄今为止没有临床意义上获益的证据。这些临床研究为其他在动物研究中有益的药物的未来试验建立了疗效评估方法。