Takeyama Ken-ichi, Ito Saya, Yamamoto Ayako, Tanimoto Hiromu, Furutani Takashi, Kanuka Hirotaka, Miura Masayuki, Tabata Tetsuya, Kato Shigeaki
Institute of Molecular and Cellular Biosciences, University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo, Japan.
Neuron. 2002 Aug 29;35(5):855-64. doi: 10.1016/s0896-6273(02)00875-9.
Spinal and bulbar muscular atrophy (SBMA) is an X-linked, adult-onset, neurodegenerative disorder affecting only males and is caused by expanded polyglutamine (polyQ) stretches in the N-terminal A/B domain of human androgen receptor (hAR). Although no overt phenotype was detected in adult fly eye photoreceptor neurons expressing mutant hAR (polyQ 52), ingestion of androgen or its known antagonists caused marked neurodegeneration with nuclear localization and structural alteration of the hAR mutant. Ligand-independent toxicity was detected with a truncated polyQ-expanded A/B domain alone, which was attenuated with cytosolic trapping by coexpression of the unliganded hAR E/F ligand binding domain. Thus, our findings suggest that the full binding of androgen to the polyQ-expanded hAR mutants leads to structural alteration with nuclear translocation that eventually results in the onset of SBMA in male patients.
脊髓延髓性肌萎缩症(SBMA)是一种X连锁的成年发病的神经退行性疾病,仅影响男性,由人类雄激素受体(hAR)N端A/B结构域中多聚谷氨酰胺(polyQ)序列扩展引起。虽然在表达突变型hAR(polyQ 52)的成年果蝇眼感光神经元中未检测到明显的表型,但摄入雄激素或其已知拮抗剂会导致显著的神经退行性变,伴有hAR突变体的核定位和结构改变。单独的截短型多聚谷氨酰胺扩展A/B结构域检测到了非配体依赖性毒性,通过共表达未结合配体的hAR E/F配体结合结构域进行胞质捕获可使其减弱。因此,我们的研究结果表明,雄激素与多聚谷氨酰胺扩展的hAR突变体的完全结合会导致结构改变和核转位,最终导致男性患者发生SBMA。