Article abstract


Nature Medicine 13, 348 - 353 (2007)
Published online: 4 March 2007 | doi:10.1038/nm1547

ASC-J9 ameliorates spinal and bulbar muscular atrophy phenotype via degradation of androgen receptor

Zhiming Yang1,2,7, Yu-Jia Chang1,3,7, I-Chen Yu1, Shuyuan Yeh1, Cheng-Chia Wu1,3, Hiroshi Miyamoto1, Diane E Merry4, Gen Sobue5, Lu-Min Chen1,6, Shu-Shi Chang1,6 & Chawnshang Chang1


Motor neuron degeneration resulting from the aggregation of the androgen receptor with an expanded polyglutamine tract (AR-polyQ) has been linked to the development of spinal and bulbar muscular atrophy (SBMA or Kennedy disease). Here we report that adding 5-hydroxy-1,7-bis(3,4-dimethoxyphenyl)-1,4,6-heptatrien-3-one (ASC-J9) disrupts the interaction between AR and its coregulators, and also increases cell survival by decreasing AR-polyQ nuclear aggregation and increasing AR-polyQ degradation in cultured cells. Intraperitoneal injection of ASC-J9 into AR-polyQ transgenic SBMA mice markedly improved disease symptoms, as seen by a reduction in muscular atrophy. Notably, unlike previous approaches in which surgical or chemical castration was used to reduce SBMA symptoms, ASC-J9 treatment ameliorated SBMA symptoms by decreasing AR-97Q aggregation and increasing VEGF164 expression with little change of serum testosterone. Moreover, mice treated with ASC-J9 retained normal sexual function and fertility. Collectively, our results point to a better therapeutic and preventative approach to treating SBMA, by disrupting the interaction between AR and AR coregulators.

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  1. George Whipple Lab for Cancer Research, Departments of Pathology, Urology, and Radiation Oncology, and The Cancer Center, University of Rochester Medical Center, Rochester, New York 14642, USA.
  2. Zhejiang University and 2nd Hospital, Hangzhou 310009, China.
  3. Taipei Medical University and Hospital, Taipei 110, Taiwan.
  4. Thomas Jefferson University, Philadelphia, Pennsylvania 19107, USA.
  5. Nagoya University, Nagoya 466-8550, Japan.
  6. China Medical University and Hospital, Taichung 404, Taiwan.
  7. These authors contributed equally to this work.

Correspondence to: Chawnshang Chang1 e-mail: chang@URMC.rochester.edu




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