The DOI matches its Crossref record; 33 of the 33 references it cites were found in a registry or an index.
4-Hydroxytamoxifen binds to and deactivates the estrogen-related receptor γ
Open accessAbstract
The estrogen-related receptors (ERRα, ERRβ, and ERRγ) form a family of orphan nuclear receptors that share significant amino acid identity with the estrogen receptors, but for which physiologic roles remain largely unknown. By using a peptide sensor assay, we have identified the stilbenes diethylstilbestrol (DES), tamoxifen (TAM), and 4-hydroxytamoxifen (4-OHT) as high-affinity ligands for ERRγ. In direct binding assays, 4-OHT had a K d value of 35 nM, and both DES and TAM displaced radiolabeled 4-OHT with K i values of 870 nM. In cell-based assays, 4-OHT binding caused a dissociation of the complex between ERRγ and the steroid receptor coactivator-1, and led to an inhibition of the constitutive transcriptional activity of ERRγ. ERRα did not bind 4-OHT, but replacing a single amino acid predicted to be in the ERRα ligand-binding pocket with the corresponding ERRγ residue allowed high-affinity 4-OHT binding. These results demonstrate the existence of high-affinity ligands for the ERR family of orphan receptors, and identify 4-OHT as a molecule that can regulate the transcriptional activity of ERRγ.
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Self-citationBile Acids: Natural Ligands for an Orphan Nuclear Receptor
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Self-citationA signature motif in transcriptional co-activators mediates binding to nuclear receptors
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Activation of the Nuclear Receptor LXR by Oxysterols Defines a New Hormone Response Pathway
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Cited by
Nuclear Receptors and Lipid Physiology: Opening the X-Files
Chawla, A., Repa, J. J., Evans, R. M., & Mangelsdorf, D. J. (2001) · Science · doi:10.1126/science.294.5548.1866 · Cited by 2,085
Schreiber, S. N., Emter, R., Hock, M. B., Knutti, D., Cardenas, J., Podvinec, M., Oakeley, E. J., & Kralli, A. (2004) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0308686101 · Cited by 658
Nuclear receptors — a perspective from Drosophila
King-Jones, K., & Thummel, C. S. (2005) · Nature Reviews Genetics · doi:10.1038/nrg1581 · Cited by 586
Jordan, V. C. (2003) · Journal of Medicinal Chemistry · doi:10.1021/jm020449y · Cited by 414
To ERR in the estrogen pathway
Giguére, V. (2002) · Trends in Endocrinology & Metabolism · doi:10.1016/s1043-2760(02)00592-1 · Cited by 401
Metadata
- Authors
- Coward, P., Lee, D., Hull, M. V., & Lehmann, J. M.
- Venue
- Proceedings of the National Academy of Sciences
- Published
- 2001-07-10
- Volume
- 98
- Issue
- 15
- Pages
- 8880-8884
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- OpenAlex
- W2150479378
- Cited by
- 265
- References
- 33
- FWCI
- 7.94
- Type
- journal article
- Language
- en
- Open access
- green
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- Coward, P., Lee, D., Hull, M. V., & Lehmann, J. M. (2001). 4-Hydroxytamoxifen binds to and deactivates the estrogen-related receptor γ. Proceedings of the National Academy of Sciences. https://doi.org/10.1073/pnas.151244398
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