Source:http://linkedlifedata.com/resource/pubmed/id/11906294
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
7
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pubmed:dateCreated |
2002-3-21
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pubmed:abstractText |
The protooncogenes Ras and Raf play important roles in signal transduction pathways regulated by mitogen-activated protein kinases. Mutations of Ras that arrest the protein in its active state are frequently implicated in tumor formation. We used Ras and Raf proteins in the yeast two-hybrid system to search for natural or synthesized substances capable of modulating Ras/Raf interaction by specifically binding to one of the interacting partners. We found that cycloalkylidene carboxylic acids enhanced Ras/Raf interaction by acting on the cysteine-rich domain of Raf. Several analogues of the active substance 2-cyclohexylidene propanoic acid were synthesized and the importance of the semicyclic double bond in the stabilization of Ras/Raf interaction was demonstrated. Variation of the size and the substituents of the cyclic system as well as the length of the carboxylic acid resulted in enhanced Ras/Raf interaction.
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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 |
Mar
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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 |
45
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1535-42
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:11906294-Amino Acid Motifs,
pubmed-meshheading:11906294-Carboxylic Acids,
pubmed-meshheading:11906294-Humans,
pubmed-meshheading:11906294-Magnetic Resonance Spectroscopy,
pubmed-meshheading:11906294-Models, Chemical,
pubmed-meshheading:11906294-Mutagenesis, Site-Directed,
pubmed-meshheading:11906294-Mutation,
pubmed-meshheading:11906294-Plasmids,
pubmed-meshheading:11906294-Protein Binding,
pubmed-meshheading:11906294-Protein Structure, Tertiary,
pubmed-meshheading:11906294-Proto-Oncogene Proteins c-raf,
pubmed-meshheading:11906294-Two-Hybrid System Techniques,
pubmed-meshheading:11906294-ras Proteins
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pubmed:year |
2002
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pubmed:articleTitle |
Synthesis and biological evaluation of cycloalkylidene carboxylic acids as novel effectors of Ras/Raf interaction.
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pubmed:affiliation |
Institut für Pharmazeutische Biologie, Universität Frankfurt/M. (Biozentrum), D-60439 Frankfurt am Main, Germany.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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