Source:http://linkedlifedata.com/resource/pubmed/id/19559507
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
11
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pubmed:dateCreated |
2009-10-9
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pubmed:abstractText |
Selective 20S proteasomal inhibition and apoptosis induction were observed when several lines of cancer cells were treated with a series of copper complexes described as [Cu(L(I))Cl] (1), [Cu(L(I))OAc] (2), and [Cu(HL(I))(L(I))]OAc (3), where HL(I) is the ligand 2,4-diiodo-6-((pyridine-2-ylmethylamino)methyl)phenol. These complexes were synthesized, characterized by means of ESI spectrometry, infrared, UV-visible and EPR spectroscopies, and X-ray diffraction when possible. After full characterization species 1-3 were evaluated for their ability to function as proteasome inhibitors and apoptosis inducers in C4-2B and PC-3 human prostate cancer cells and MCF-10A normal cells. With distinct stoichiometries and protonation states, this series suggests the assignment of species [CuL(I)](+) as the minimal pharmacophore needed for proteasomal chymotryspin-like activity inhibition and permits some initial inference of mechanistic information.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
1768-3254
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:volume |
44
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4353-61
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pubmed:dateRevised |
2011-5-10
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pubmed:meshHeading |
pubmed-meshheading:19559507-Antineoplastic Agents,
pubmed-meshheading:19559507-Apoptosis,
pubmed-meshheading:19559507-Cell Line,
pubmed-meshheading:19559507-Cell Line, Tumor,
pubmed-meshheading:19559507-Cell Survival,
pubmed-meshheading:19559507-Copper,
pubmed-meshheading:19559507-Humans,
pubmed-meshheading:19559507-Male,
pubmed-meshheading:19559507-Models, Molecular,
pubmed-meshheading:19559507-Molecular Structure,
pubmed-meshheading:19559507-Phenols,
pubmed-meshheading:19559507-Prostatic Neoplasms,
pubmed-meshheading:19559507-Proteasome Endopeptidase Complex
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pubmed:year |
2009
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pubmed:articleTitle |
Metals in anticancer therapy: copper(II) complexes as inhibitors of the 20S proteasome.
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pubmed:affiliation |
Department of Chemistry, Wayne State University, Detroit, MI 48202, USA.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, Non-P.H.S.,
Research Support, Non-U.S. Gov't,
Research Support, N.I.H., Extramural
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