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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
14
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pubmed:dateCreated |
2005-6-30
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pubmed:abstractText |
[structure: see text] (-)-16-Normethyldictyostatin has been made by total synthesis and is a potent antitumor agent in cells expressing wild-type tubulin and in one mutant cell line that is resistant to paclitaxel, but it is much less active than dictyostatin in another paclitaxel-resistant cell line where Val is substituted for Phe270. This provides strong evidence that the C16 methyl group of the dictyostatins is oriented toward Phe270 in the paclitaxel-binding site on beta-tubulin.
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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 |
1523-7060
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
7
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pubmed:volume |
7
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2873-6
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:15987158-Animals,
pubmed-meshheading:15987158-Antineoplastic Agents,
pubmed-meshheading:15987158-Brain,
pubmed-meshheading:15987158-Cattle,
pubmed-meshheading:15987158-Drug Resistance, Neoplasm,
pubmed-meshheading:15987158-Drug Screening Assays, Antitumor,
pubmed-meshheading:15987158-Macrolides,
pubmed-meshheading:15987158-Molecular Structure,
pubmed-meshheading:15987158-Paclitaxel,
pubmed-meshheading:15987158-Phenylalanine,
pubmed-meshheading:15987158-Stereoisomerism,
pubmed-meshheading:15987158-Structure-Activity Relationship,
pubmed-meshheading:15987158-Tubulin,
pubmed-meshheading:15987158-Valine
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pubmed:year |
2005
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pubmed:articleTitle |
Synthesis and biological evaluation of (-)-16-normethyldictyostatin: a potent analogue of (-)-dictyostatin.
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pubmed:affiliation |
Department of Chemistry, University of Pittsburgh, Pennsylvania 15261, USA.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, N.I.H., Extramural
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