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rdf:type |
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lifeskim:mentions |
|
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pubmed:issue |
16
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pubmed:dateCreated |
2002-7-25
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pubmed:abstractText |
Several 2-(arylamino)pyrimidine-5-carboxylic acids were designed as novel retinoid X receptor (RXR) antagonists. Compound 6a or 6b alone did not exhibit differentiation-inducing activity toward HL-60 cells and did not affect the activity of a retinoic acid receptor (RAR) agonist, Am80, but did inhibit the synergistic activity of an RXR agonist, PA024 (3), in the presence of Am80. The activity of 6 was ascribed to selective antagonism at the RXR site of RXR-RAR heterodimers.
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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 |
Aug
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
1
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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 |
3327-30
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:12139443-Benzoates,
pubmed-meshheading:12139443-Carboxylic Acids,
pubmed-meshheading:12139443-Cell Differentiation,
pubmed-meshheading:12139443-Depression, Chemical,
pubmed-meshheading:12139443-Dimerization,
pubmed-meshheading:12139443-HL-60 Cells,
pubmed-meshheading:12139443-Humans,
pubmed-meshheading:12139443-Pyrimidines,
pubmed-meshheading:12139443-Receptors, Retinoic Acid,
pubmed-meshheading:12139443-Retinoid X Receptors,
pubmed-meshheading:12139443-Structure-Activity Relationship,
pubmed-meshheading:12139443-Tetrahydronaphthalenes,
pubmed-meshheading:12139443-Transcription Factors
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pubmed:year |
2002
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pubmed:articleTitle |
Novel retinoid X receptor antagonists: specific inhibition of retinoid synergism in RXR-RAR heterodimer actions.
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pubmed:affiliation |
Graduate School of Pharmaceutical Sciences, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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