Department of Neurology, Nagoya University Graduate School of Medicine, 65 Tsurumai-cho, Showa-ku, Nagoya 466-8550, Japan.
Neural Plast. 2012;2012:369284. doi: 10.1155/2012/369284. Epub 2012 Jun 7.
Spinal and bulbar muscular atrophy (SBMA) is the first member identified among polyglutamine diseases characterized by slowly progressive muscle weakness and atrophy of the bulbar, facial, and limb muscles pathologically associated with motor neuron loss in the spinal cord and brainstem. Androgen receptor (AR), a disease-causing protein of SBMA, is a well-characterized ligand-activated transcription factor, and androgen binding induces nuclear translocation, conformational change and recruitment of coregulators for transactivation of AR target genes. Some therapeutic strategies for SBMA are based on these native functions of AR. Since ligand-induced nuclear translocation of mutant AR has been shown to be a critical step in motor neuron degeneration in SBMA, androgen deprivation therapies using leuprorelin and dutasteride have been developed and translated into clinical trials. Although the results of these trials are inconclusive, renewed clinical trials with more sophisticated design might prove the effectiveness of hormonal intervention in the near future. Furthermore, based on the normal function of AR, therapies targeted for conformational changes of AR including amino-terminal (N) and carboxy-terminal (C) (N/C) interaction and transcriptional coregulators might be promising. Other treatments targeted for mitochondrial function, ubiquitin-proteasome system (UPS), and autophagy could be applicable for all types of polyglutamine diseases.
脊髓延髓肌肉萎缩症(SBMA)是聚谷氨酰胺疾病中第一个被鉴定的成员,其特征是肌肉无力和进行性萎缩,主要影响延髓、面部和肢体肌肉,病理上与脊髓和脑干中的运动神经元丧失有关。SBMA 的致病蛋白雄激素受体(AR)是一种特征明确的配体激活转录因子,雄激素结合诱导核易位、构象变化,并募集 AR 靶基因转录激活的共激活因子。一些 SBMA 的治疗策略基于 AR 的这些天然功能。由于已经表明突变型 AR 的配体诱导核易位是 SBMA 中运动神经元退化的关键步骤,因此已经开发了使用亮丙瑞林和度他雄胺的去势治疗,并转化为临床试验。尽管这些试验的结果尚无定论,但具有更复杂设计的新临床试验可能在不久的将来证明激素干预的有效性。此外,基于 AR 的正常功能,针对 AR 的构象变化的治疗方法,包括氨基末端(N)和羧基末端(C)(N/C)相互作用和转录共激活因子,可能具有前景。针对线粒体功能、泛素-蛋白酶体系统 (UPS) 和自噬的其他治疗方法可能适用于所有类型的聚谷氨酰胺疾病。