| Disulfiram, and disulfiram derivatives as novel potential anticancer drugs targeting the ubiquitin-proteasome system in both preclinical and clinical studies. | |
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MedLine Citation:
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PMID: 21247383 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Disulfiram is a FDA approved drug for the treatment of alcoholism and available for clinical use since over 5 decades. Despite data from the 1970s and 80s that showed that disulfiram and analogs are able to enhance the activity of anticancer cytotoxic drugs and might be useful chemopreventative agents, the underlying molecular mechanisms remained unknown until recently. Large scale screening efforts for agents that can inhibit the proteasome and be used as novel anticancer drugs, revealed that disulfiram has proteasome inhibitory activity. Moreover, disulfiram was also found to have specific activity against zinc fingers and RING-finger ubiquitin E3 ligases that play an important role in cancer development. Here, we review the preclinical and clinical studies exploring disulfiram as an anticancer agent as well as research programs that focus on the development of disulfiram derivatives as inhibitors of the ubiquitin-proteasome system. |
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Authors:
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F R Kona; D Buac; A M Burger |
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Publication Detail:
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Type: Journal Article; Research Support, N.I.H., Extramural; Review |
Journal Detail:
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Title: Current cancer drug targets Volume: 11 ISSN: 1873-5576 ISO Abbreviation: Curr Cancer Drug Targets Publication Date: 2011 Mar |
Date Detail:
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Created Date: 2011-03-14 Completed Date: 2011-07-07 Revised Date: 2012-08-20 |
Medline Journal Info:
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Nlm Unique ID: 101094211 Medline TA: Curr Cancer Drug Targets Country: Netherlands |
Other Details:
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Languages: eng Pagination: 338-46 Citation Subset: IM |
Affiliation:
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Barbara Ann Karmanos Cancer Institute and Department of Pharmacology, Wayne State University School of Medicine, Detroit, MI, USA. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Antineoplastic Agents / therapeutic use* Clinical Trials as Topic Disulfiram / therapeutic use* Drug Evaluation, Preclinical Humans Neoplasms / drug therapy*, metabolism Protease Inhibitors / therapeutic use* Proteasome Endopeptidase Complex / drug effects* |
| Grant Support | |
ID/Acronym/Agency:
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R01CA127258/CA/NCI NIH HHS |
| Chemical | |
Reg. No./Substance:
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0/Antineoplastic Agents; 0/Protease Inhibitors; 97-77-8/Disulfiram; EC 3.4.25.1/Proteasome Endopeptidase Complex |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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