Source:http://linkedlifedata.com/resource/pubmed/id/15501068
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
23
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pubmed:dateCreated |
2004-10-25
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pubmed:abstractText |
We designed and synthesized novel retinoid X receptor (RXR)-selective antagonists bearing a carborane moiety. Compounds 8a-d or 9a-d themselves have no differentiation-inducing activity toward HL-60 cells and no inhibitory activity towards a retinoic acid receptor (RAR) agonist. However, they inhibit the synergistic activity of an RXR agonist, PA024, in the presence of Am80 on the cell differentiation of HL-60. Transactivation assay using RARs and RXRs suggested that the inhibitory activity of 9b resulted from the selective antagonism at the RXR site of RXR-RAR heterodimers.
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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 |
Dec
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pubmed:issn |
0960-894X
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
6
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pubmed:volume |
14
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
5913-8
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:15501068-Boron Compounds,
pubmed-meshheading:15501068-Cell Differentiation,
pubmed-meshheading:15501068-Dose-Response Relationship, Drug,
pubmed-meshheading:15501068-HL-60 Cells,
pubmed-meshheading:15501068-Humans,
pubmed-meshheading:15501068-Hydrophobic and Hydrophilic Interactions,
pubmed-meshheading:15501068-Retinoid X Receptors
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pubmed:year |
2004
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pubmed:articleTitle |
Novel retinoid X receptor (RXR) antagonists having a dicarba-closo-dodecaborane as a hydrophobic moiety.
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pubmed:affiliation |
Faculty of Pharmaceutical Sciences, Tohoku Pharmaceutical University, 4-4-1, Komatsushima, Aoba-ku, Sendai 981-8558, Japan.
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pubmed:publicationType |
Journal Article
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