The DOI matches its Crossref record; 102 of the 102 references it cites were found in a registry or an index.
Estrogen receptor transcription and transactivation Estrogen receptor alpha and estrogen receptor beta: regulation by selective estrogen receptor modulators and importance in breast cancer
Open accessAbstract
Estrogens display intriguing tissue-selective action that is of great biomedical importance in the development of optimal therapeutics for the prevention and treatment of breast cancer, for menopausal hormone replacement, and for fertility regulation. Certain compounds that act through the estrogen receptor (ER), now referred to as selective estrogen receptor modulators (SERMs), can demonstrate remarkable differences in activity in the various estrogen target tissues, functioning as agonists in some tissues but as antagonists in others. Recent advances elucidating the tripartite nature of the biochemical and molecular actions of estrogens provide a good basis for understanding these tissue-selective actions. As discussed in this thematic review, the development of optimal SERMs should now be viewed in the context of two estrogen receptor subtypes, ERalpha and ERbeta, that have differing affinities and responsiveness to various SERMs, and differing tissue distribution and effectiveness at various gene regulatory sites. Cellular, biochemical, and structural approaches have also shown that the nature of the ligand affects the conformation assumed by the ER-ligand complex, thereby regulating its state of phosphorylation and the recruitment of different coregulator proteins. Growth factors and protein kinases that control the phosphorylation state of the complex also regulate the bioactivity of the ER. These interactions and changes determine the magnitude of the transcriptional response and the potency of different SERMs. As these critical components are becoming increasingly well defined, they provide a sound basis for the development of novel SERMs with optimal profiles of tissue selectivity as medical therapeutic agents.
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Sex differences in pain and analgesia: the role of gonadal hormones
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Fulvestrant: an oestrogen receptor antagonist with a novel mechanism of action
Osborne, C. K., Wakeling, A., & Nicholson, R. I. (2004) · British Journal of Cancer · doi:10.1038/sj.bjc.6601629 · Cited by 414
Critchley, H. O. D., Henderson, T. A., Kelly, R. W., Scobie, G. S., Evans, L. R., Groome, N. P., & Saunders, P. T. K. (2002) · The Journal of Clinical Endocrinology & Metabolism · doi:10.1210/jc.2002-020502 · Cited by 87
Actions of 17β-estradiol and testosterone in the mitochondria and their implications in aging
Vasconsuelo, A., Milanesi, L., & Boland, R. (2013) · Ageing Research Reviews · doi:10.1016/j.arr.2013.09.001 · Cited by 55
Xie, B., Yin, Z., Hu, Z., Lv, J., Du, C., Deng, X., Huang, Y., Li, Q., Huang, J., Liang, K., et al. (2023) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c02032 · Cited by 39
Metadata
- Authors
- Katzenellenbogen, B. S., & Katzenellenbogen, J. A.
- Venue
- Breast Cancer Research
- Published
- 2000-10
- Volume
- 2
- Issue
- 5
- Pages
- 335-44
- ISSN
- 1465-5411 (ISSN-L)
- 1465-542X
- OpenAlex
- W2126824378
- Cited by
- 293
- References
- 102
- FWCI
- 6.12
- Type
- journal article
- Language
- en
- Open access
- gold
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- Katzenellenbogen, B. S., & Katzenellenbogen, J. A. (2000). Estrogen receptor transcription and transactivation Estrogen receptor alpha and estrogen receptor beta: regulation by selective estrogen receptor modulators and importance in breast cancer. Breast Cancer Research. https://doi.org/10.1186/bcr78
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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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