The DOI matches its Crossref record; 2 of the 2 references it cites were found in a registry or an index.
Antiestrogen ICI 164,384 reduces cellular estrogen receptor content by increasing its turnover.
Open accessAbstract
The ability of estrogens to stimulate the transcriptional activity of the estrogen receptor can be inhibited by a diverse range of estrogen antagonists. Here we show that the antiestrogen ICI 164,384, N-(n-butyl)-11-[3,17 beta-dihydroxy-estra-1,3,5(10)-trien-7 alpha-yl]N-methylundecanamide, rapidly reduces the levels of receptor protein transiently expressed in cells without affecting receptor mRNA abundance. The reduction in the levels of receptor protein is dose dependent, reversible by estradiol, and mediated by the hormone-binding domain of the receptor. Pulse-chase experiments indicate that the half-life of the receptor is reduced from approximately 5 hr in the presence of estradiol to less than 1 hr by ICI 164,384. A similar reduction in estrogen receptor levels is demonstrated in human breast cancer cells treated with ICI 164,384. We discuss the possibility that the increased turnover of the receptor might be a consequence of impaired receptor dimerization.
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Cites
Gene regulation by steroid hormones
Beato, M. (1989) · Cell · doi:10.1016/0092-8674(89)90237-7 · Cited by 3,383
Novel steroidal pure antiestrogens
Bowler, J., Lilley, T. J., Pittam, J. D., & Wakeling, A. E. (1989) · Steroids · doi:10.1016/0039-128x(89)90076-7 · Cited by 206
Cited by
Induced protein degradation: an emerging drug discovery paradigm
Lai, A. C., & Crews, C. M. (2017) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2016.211 · Cited by 1,486
Coregulator Function: A Key to Understanding Tissue Specificity of Selective Receptor Modulators
Smith, C. L., & O’Malley, B. W. (2004) · Endocrine Reviews · doi:10.1210/er.2003-0023 · Cited by 931
Reid, G., Hübner, M. R., Métivier, R., Brand, H., Denger, S., Manu, D., Beaudouin, J., Ellenberg, J., & Gannon, F. (2003) · Molecular Cell · doi:10.1016/s1097-2765(03)00090-x · Cited by 732
The antiestrogen ICI 182780 disrupts estrogen receptor nucleocytoplasmic shuttling
Dauvois, S., White, R., & Parker, M. G. (1993) · Journal of Cell Science · doi:10.1242/jcs.106.4.1377 · Cited by 522
Self-citationAnalysis of estrogen receptor function in vitro reveals three distinct classes of antiestrogens
McDonnell, D. P. (1995) · Molecular Endocrinology · doi:10.1210/me.9.6.659 · Cited by 526
Metadata
- Authors
- Dauvois, S., Danielian, P. S., White, R., & Parker, M. G.
- Venue
- Proceedings of the National Academy of Sciences
- Published
- 1992-05
- Volume
- 89
- Issue
- 9
- Pages
- 4037-4041
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- OpenAlex
- W2148307287
- Cited by
- 465
- References
- 2
- FWCI
- 12.89
- Type
- journal article
- Language
- en
- Open access
- green
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- Dauvois, S., Danielian, P. S., White, R., & Parker, M. G. (1992). Antiestrogen ICI 164,384 reduces cellular estrogen receptor content by increasing its turnover. Proceedings of the National Academy of Sciences. https://doi.org/10.1073/pnas.89.9.4037
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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