A bis-Benzylidine Piperidone Targeting Proteasome Ubiquitin Receptor RPN13/ADRM1 as a Therapy for Cancer

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 sensiti...

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Veröffentlicht in:	Cancer cell 2013-12, Vol.24 (6), p.791-805
Hauptverfasser:	Anchoori, Ravi K., Karanam, Balasubramanyam, Peng, Shiwen, Wang, Joshua W., Jiang, Rosie, Tanno, Toshihiko, Orlowski, Robert Z., Matsui, William, Zhao, Ming, Rudek, Michelle A., Hung, Chien-fu, Chen, Xiang, Walters, Kylie J., Roden, Richard B.S.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Boronic Acids - pharmacology Bortezomib Cell Line, Tumor Endoplasmic Reticulum Stress Female Genes, p53 Humans Membrane Glycoproteins - antagonists & inhibitors Membrane Glycoproteins - chemistry Membrane Glycoproteins - physiology Mice Mice, Inbred BALB C Mice, Inbred C57BL Neoplasms - drug therapy Neoplasms - pathology Piperidones - pharmacology Proteasome Inhibitors - pharmacokinetics Proteasome Inhibitors - pharmacology Pyrazines - pharmacology Ubiquitination
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