Source:http://linkedlifedata.com/resource/pubmed/id/18215015
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4
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pubmed:dateCreated |
2008-2-21
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pubmed:abstractText |
Aurora kinases are essential for chromosomal segregation and cell division and thereby important for maintaining the proper genomic integrity. There are three classes of aurora kinases in humans: A, B, and C. Aurora kinase A is frequently overexpressed in various cancers. The link of the overexpression and tumorigenesis is yet to be understood. By employing virtual screening, we have found that anacardic acid, a pentadecane aliphatic chain containing hydroxylcarboxylic acid, from cashew nut shell liquid could be docked in Aurora kinases A and B. Remarkably, we found that anacardic acid could potently activate the Aurora kinase A mediated phosphorylation of histone H3, but at a similar concentration the activity of aurora kinase B remained unaffected in vitro. Mechanistically, anacardic acid induces the structural changes and also the autophosphorylation of the aurora kinase A to enhance the enzyme activity. This data thus indicate anacardic acid as the first small-molecule activator of Aurora kinase, which could be highly useful for probing the function of hyperactive (overexpressed) Aurora kinase A.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Anacardic Acids,
http://linkedlifedata.com/resource/pubmed/chemical/Enzyme Activators,
http://linkedlifedata.com/resource/pubmed/chemical/Histones,
http://linkedlifedata.com/resource/pubmed/chemical/Protein-Serine-Threonine Kinases,
http://linkedlifedata.com/resource/pubmed/chemical/anacardic acid,
http://linkedlifedata.com/resource/pubmed/chemical/aurora kinase
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
28
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pubmed:volume |
51
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
792-7
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pubmed:dateRevised |
2011-7-11
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pubmed:meshHeading |
pubmed-meshheading:18215015-Anacardic Acids,
pubmed-meshheading:18215015-Anacardium,
pubmed-meshheading:18215015-Cell Line,
pubmed-meshheading:18215015-Cloning, Molecular,
pubmed-meshheading:18215015-Crystallography, X-Ray,
pubmed-meshheading:18215015-Enzyme Activators,
pubmed-meshheading:18215015-Histones,
pubmed-meshheading:18215015-Humans,
pubmed-meshheading:18215015-Kinetics,
pubmed-meshheading:18215015-Models, Molecular,
pubmed-meshheading:18215015-Molecular Structure,
pubmed-meshheading:18215015-Phosphorylation,
pubmed-meshheading:18215015-Protein-Serine-Threonine Kinases,
pubmed-meshheading:18215015-Spectrometry, Fluorescence
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pubmed:year |
2008
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pubmed:articleTitle |
Specific small-molecule activator of Aurora kinase A induces autophosphorylation in a cell-free system.
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pubmed:affiliation |
Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore 06, India.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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