Retinyl Methyl Ether: Binding to Transport Proteins and Effect on Transcriptional Regulation
| Autor: | Brahma P. Sani, Xiao-kun Zhang, Donald L. Hill, Y. Fulmer Shealy |
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| Rok vydání: | 1996 |
| Předmět: |
Transcription
Genetic Macromolecular Substances Receptors Retinoic Acid medicine.drug_class Biophysics Retinoic acid Biology Retinoid X receptor Transfection Biochemistry Cell Line chemistry.chemical_compound Chlorocebus aethiops medicine Transcriptional regulation Animals Anticarcinogenic Agents Retinoid Vitamin A Receptor Molecular Biology Cell Nucleus Expression vector Retinoic Acid Receptor alpha Mammary Neoplasms Experimental Retinol-Binding Proteins Cellular Cell Biology Molecular biology Recombinant Proteins Rats Transport protein Retinol-Binding Proteins Retinoic acid receptor Retinoid X Receptors chemistry Female Protein Multimerization Transcription Factors |
| Zdroj: | Biochemical and Biophysical Research Communications. 223:293-298 |
| ISSN: | 0006-291X |
| DOI: | 10.1006/bbrc.1996.0887 |
| Popis: | Retinyl methyl ether (RME) which prevents cancers of the rat mammary gland, binds to cellular retinol-binding protein and serum retinol-binding protein but not to cellular retinoic acid-binding protein or to the nuclear retinoid receptors, RARs/RXRs. Since the biochemical effects of retinoids likely involve activation or suppression of RAR/RXR-mediated gene transcription, we evaluated such activity of RME by performing cotransfection assays involving CV-1 cells, expression vectors containing RAR and/or RXR cDNA, and an appropriate reporter vector. In the concentration range of 10(-9)-10(-6), RME did not activate transcription by either of the heterodimers (RARalpha, beta or gamma/RXR alpha) or the homodimer (RARalpha/RARalpha). The retinoid, however, exhibited concentration-dependent inhibitory effects on the basal level of transcriptional activity (no other retinoid added) of both the RAR beta- and RARgamma/RXRalpha heterodimers and of the retinoic acid-induced transcriptional activation of the RARgamma/RXRalpha receptors. Thus, RME acted as a retinoic acid antagonist, a role possibly involved in its cancer preventive activity. |
| Databáze: | OpenAIRE |
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