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Type: Journal article
Title: Use of [¹²⁵I]4'-iodoflavone as a tool to characterize ligand-dependent differences in Ah receptor behavior
Other Titles: Use of [(125)I]4'-iodoflavone as a tool to characterize ligand-dependent differences in Ah receptor behavior
Author: Swanson, H.
Whitelaw, M.
Petrulis, J.
Perdew, G.
Citation: Journal of Biochemical and Molecular Toxicology, 2002; 16(6):298-310
Publisher: John Wiley & Sons Inc
Issue Date: 2002
ISSN: 1095-6670
Organisation: Centre for the Molecular Genetics of Development
Statement of
Hollie I. Swanson, Murray L. Whitelaw, John R. Petrulis, Gary H. Perdew
Abstract: We have synthesized [(125)I]4'-iodoflavone to study Ah receptor (AhR)-ligand interactions by a class of AhR ligands distinct from the prototypic ligand 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD). This radioligand allows the comparison of AhR-ligand interactions using a ligand that differs in AhR affinity, and yet has the same radiospecific activity as [(125)I]2-iodo-7,8-dibromodibenzo-p-dioxin. Specific binding of [(125)I]4'-iodoflavone with the AhR was detected as a single radioactive peak ( approximately 9.7 S) following density sucrose gradient analysis. Cytosolic extracts from both Hepa 1 and HeLa cells were used as the source of mouse and human AhR, respectively. A approximately 6.7 S form of radioligand-bound Ah receptor was detected in the high salt nuclear extracts of both cell lines. In HeLa cells approximately twofold more [(125)I]4'-iodoflavone-AhR 6 S complex, compared with [(125)I]2-iodo-7,8-dibromodibenzo-p-dioxin, was recovered in nuclear extracts. A comparison of the ability of 4'-iodoflavone and TCDD to cause time-dependent translocation of AhR-yellow fluorescent protein revealed that 4'-iodoflavone was more efficient at enhancing nuclear accumulation of the receptor. These results suggest that [(125)I]4'-iodoflavone is a particularly useful and easily synthesized ligand for studying the AhR.
Keywords: Hela Cells
Tumor Cells, Cultured
Iodine Radioisotopes
Bacterial Proteins
Luminescent Proteins
Nuclear Proteins
Receptors, Aryl Hydrocarbon
Spectrometry, Fluorescence
Binding, Competitive
Protein Transport
Polychlorinated Dibenzodioxins
Description: The definitive version may be found at
DOI: 10.1002/jbt.10053
Published version:
Appears in Collections:Aurora harvest 2
Centre for the Molecular Genetics of Development publications
Molecular and Biomedical Science publications

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