A bis-benzylidine piperidone targeting proteasome ubiquitin receptor RPN13/ADRM1 as a therapy for cancer.

@article{Anchoori2013ABP,
  title={A bis-benzylidine piperidone targeting proteasome ubiquitin receptor RPN13/ADRM1 as a therapy for cancer.},
  author={Ravi Kumar Anchoori and Balasubramanyam Karanam and Shiwen Peng and Joshua Weiyuan Wang and Rosie T Jiang and Toshihiko Tanno and Robert Z Orlowski and William Matsui and Ming Zhao and Michelle A. Rudek and Chien-Fu Hung and Xiang Chen and Kylie J. Walters and Richard B S Roden},
  journal={Cancer cell},
  year={2013},
  volume={24 6},
  pages={
          791-805
        }
}
The bis-benzylidine piperidone RA190 covalently binds to cysteine 88 of ubiquitin receptor RPN13 in the 19S regulatory particle and inhibits proteasome function, triggering rapid accumulation of polyubiquitinated proteins. Multiple myeloma (MM) lines, even those resistant to bortezomib, were sensitive to RA190 via endoplasmic reticulum stress-related apoptosis. RA190 stabilized targets of human papillomavirus (HPV) E6 oncoprotein, and preferentially killed HPV-transformed cells. After oral or… CONTINUE READING
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