| Retinoid agonist activities of synthetic geranyl geranoic acid derivatives. | |
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MedLine Citation:
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PMID: 7726866 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Micromolar concentrations of 4,5- didehydro geranyl geranoic acid (GGA) were able to induce up-regulation of retinoic acid receptor-beta gene expression in human hepatoma-derived cell line, HuH-7, to the same extent as all-trans RA. In chloramphenicol acetyl transferase (CAT) assay with retinoic acid response element-beta, GGA and 4,5-didehydro GGA were both positive, but 2,3-dihydro GGA was negative, even though these GGA derivatives have been reported to be all potent ligands for cellular retinoic-acid-binding protein(CRABP). However, 10,11,14,15- tetrahydro- 4,5- didehydro GGA, a compound without any affinity for CRABP, transactivated CAT gene expression. On the other hand, only GGA and 4,5-didehydro GGA were active to induce CAT gene expression through retinoid X response element of cellular retinol binding protein, type II gene. We show for the first time that chemically synthesized acyclic organic acids are potential agonists of natural retinoids. |
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Authors:
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H Araki; Y Shidoji; Y Yamada; H Moriwaki; Y Muto |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Biochemical and biophysical research communications Volume: 209 ISSN: 0006-291X ISO Abbreviation: Biochem. Biophys. Res. Commun. Publication Date: 1995 Apr |
Date Detail:
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Created Date: 1995-05-25 Completed Date: 1995-05-25 Revised Date: 2004-11-17 |
Medline Journal Info:
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Nlm Unique ID: 0372516 Medline TA: Biochem Biophys Res Commun Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 66-72 Citation Subset: IM |
Affiliation:
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First Department of Internal Medicine, Gifu University School of Medicine, Japan. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Chloramphenicol O-Acetyltransferase
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genetics Diterpenes / chemistry, pharmacology* Gene Expression Regulation / drug effects Humans Receptors, Retinoic Acid / genetics Retinoids / agonists*, pharmacology Tumor Cells, Cultured |
| Chemical | |
Reg. No./Substance:
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0/Diterpenes; 0/Receptors, Retinoic Acid; 0/Retinoids; 0/retinoic acid binding protein II, cellular; 0/retinoic acid receptor beta; 83807-40-3/geranylgeranic acid; EC 2.3.1.28/Chloramphenicol O-Acetyltransferase |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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