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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
13
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pubmed:dateCreated |
2011-7-7
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pubmed:abstractText |
A series of flavone analogues were synthesized and evaluated for their antiproliferation activity against breast cancer cells. The IC(50) of compound 10 and 24 were determined to be at 5 ?M. These compounds were used as baits to screen breast cancer cDNA expression phage display proteome library. DNA sequencing of the binding phages suggests that eEF1A1 is a target protein for 10 and 24. Further optimization of these compounds led to the discovery of 39 with higher cytotoxic potency (IC(50) = 1 ?M) and binding to eEF1A2. Biological and biochemical data suggest that eEF1A2 might be a therapeutic target and that 39 is an excellent lead compound for further development.
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pubmed:grant |
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
1520-4804
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pubmed:author |
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pubmed:issnType |
Electronic
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pubmed:day |
14
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pubmed:volume |
54
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4339-49
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pubmed:dateRevised |
2011-9-26
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pubmed:meshHeading |
pubmed-meshheading:21599001-Antineoplastic Agents,
pubmed-meshheading:21599001-Bacteriophage T7,
pubmed-meshheading:21599001-Breast Neoplasms,
pubmed-meshheading:21599001-Cell Line, Tumor,
pubmed-meshheading:21599001-Drug Screening Assays, Antitumor,
pubmed-meshheading:21599001-Female,
pubmed-meshheading:21599001-Flavones,
pubmed-meshheading:21599001-Humans,
pubmed-meshheading:21599001-Imidazoles,
pubmed-meshheading:21599001-Neoplasms, Hormone-Dependent,
pubmed-meshheading:21599001-Peptide Elongation Factor 1,
pubmed-meshheading:21599001-Peptide Library,
pubmed-meshheading:21599001-Protein Binding,
pubmed-meshheading:21599001-Proteome,
pubmed-meshheading:21599001-Receptors, Estrogen,
pubmed-meshheading:21599001-Stereoisomerism,
pubmed-meshheading:21599001-Structure-Activity Relationship,
pubmed-meshheading:21599001-Surface Plasmon Resonance
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pubmed:year |
2011
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pubmed:articleTitle |
Novel flavonoids with antiproliferative activities against breast cancer cells.
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pubmed:affiliation |
Department of Biochemistry and Molecular Medicine, University of California Davis, Sacramento, California 95817, United States.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, Non-P.H.S.,
Research Support, N.I.H., Extramural
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