Reversible inhibitor of p97, DBeQ, impairs both ubiquitin-dependent and autophagic protein clearance pathways

A specific small-molecule inhibitor of p97 would provide an important tool to investigate diverse functions of this essential ATPase associated with diverse cellular activities (AAA) ATPase and to evaluate its potential to be a therapeutic target in human disease. We carried out a high-throughput sc...

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Veröffentlicht in:	Proceedings of the National Academy of Sciences - PNAS 2011-03, Vol.108 (12), p.4834-4839
Hauptverfasser:	Chou, Tsui-Fen, Brown, Steve J., Minond, Dmitriy, Nordin, Brian E., Li, Kelin, Jones, Amanda C., Chase, Peter, Porubsky, Patrick R., Stoltz, Brian M., Schoenen, Frank J., Patricelli, Matthew P., Hodder, Peter, Rosen, Hugh, Deshaies, Raymond J., King, Randy
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenosine triphosphatase Adenosine triphosphatases Adenosine Triphosphatases - antagonists & inhibitors Adenosine Triphosphatases - genetics Adenosine Triphosphatases - metabolism Animals Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Apoptosis Autophagy - drug effects Biological Sciences Cancer Cancer therapies Caspase 3 - genetics Caspase 3 - metabolism Caspase 7 - genetics Caspase 7 - metabolism Cell death Cell growth Cell Line Cell lines Endoplasmic Reticulum - enzymology Endoplasmic Reticulum - genetics Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology HEK293 cells HeLa cells Humans Inhibitory concentration 50 Mice Molecules Neoplasms - drug therapy Neoplasms - enzymology Nuclear Proteins - antagonists & inhibitors Nuclear Proteins - genetics Nuclear Proteins - metabolism Physical Sciences Proteasome Endopeptidase Complex - genetics Proteasome Endopeptidase Complex - metabolism Proteins Quinazolines - chemical synthesis Quinazolines - chemistry Quinazolines - pharmacology Ribonucleic acid RNA Small interfering RNA Substrates Ubiquitin - genetics Ubiquitin - metabolism Ubiquitins
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