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Endocrine Pharmacology of Antiestrogens as Antitumor Agents*
Abstract
IN 1958, Lerner and co-workers (1) described the biological properties of the first nonsteroidal antiestrogen MER25 (see Fig. 1). The discovery of this new class of drugs opened up a variety of clinical possibilities (2, 3), but early studies were terminated because of toxic side effects. Another member of this new class of drugs, clomiphene (then known as chloramiphene or MRL41), held the promise of being a potential antifertility agent (4); however, clinical studies demonstrated that ovulation was induced (5). The drug is now available as a profertility agent in subfertile women (6). During the 1960s a range of antiestrogens was synthesized by the pharmaceutical industry for potential applications in gynecology (7, 8). In the main though, these agents were used only to study reproductive endocrinology in the laboratory. However the focus of clinical application slowly changed from the broad market of contraception to the relatively small market of advanced breast cancer therapy.
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Citations
Cited by
(1991) · PubMed · Cited by 1,101
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
Jordan, V. C. (2003) · Journal of Medicinal Chemistry · doi:10.1021/jm020449y · Cited by 414
Self-citationMontano, M. M., Ekena, K., Delage-Mourroux, R., Chang, W., Martini, P., & Katzenellenbogen, B. S. (1999) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.96.12.6947 · Cited by 296
Molecular Mechanisms of Estrogen Action: Selective Ligands and Receptor Pharmacology
Katzenellenbogen, B. S., Choi, I., Delage-Mourroux, R., Ediger, T. R., Martini, P. G. V., Montano, M., Sun, J., Weis, K., & Katzenellenbogen, J. A. (2000) · The Journal of Steroid Biochemistry and Molecular Biology · doi:10.1016/s0960-0760(00)00104-7 · Cited by 289
Metadata
- Authors
- JORDAN, V. C., & MURPHY, C. S.
- Venue
- Endocrine Reviews
- Publisher
- The Endocrine Society
- Published
- 1990-11
- Volume
- 11
- Issue
- 4
- Pages
- 578-610
- ISSN
- 0163-769X (ISSN-L)
- 1945-7189
- OpenAlex
- W2057700119
- Cited by
- 400
- References
- 0
- FWCI
- 15.12
- Type
- journal article
- Language
- en
- Open access
- closed
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- JORDAN, V. C., & MURPHY, C. S. (1990). Endocrine Pharmacology of Antiestrogens as Antitumor Agents*. Endocrine Reviews. https://doi.org/10.1210/edrv-11-4-578
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
