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Nonsteroidal estrogen

Topic: Biology

 From HandWiki - Reading time: 7 min

Short description: Class of drugs
Nonsteroidal estrogen
Drug class
Diethylstilbestrol, one of the most well-known nonsteroidal estrogens.
Class identifiers
SynonymsNonsteroidal estrogen receptor agonists
ATC codeG03C
Biological targetEstrogen receptors (ERα, ERβ, mERs (e.g., GPER, others))
Chemical classNonsteroidal

A nonsteroidal estrogen is an estrogen with a nonsteroidal chemical structure.[1] The most well-known example is the stilbestrol estrogen diethylstilbestrol (DES).[1][2] Although nonsteroidal estrogens formerly had an important place in medicine, they have gradually fallen out of favor following the discovery of toxicities associated with high-dose DES starting in the early 1970s, and are now almost never used.[2][3][4] On the other hand, virtually all selective estrogen receptor modulators (SERMs) are nonsteroidal, with triphenylethylenes like tamoxifen and clomifene having been derived from DES,[5] and these drugs remain widely used in medicine for the treatment of breast cancer among other indications.[6] In addition to pharmaceutical drugs, many xenoestrogens, including phytoestrogens, mycoestrogens, and synthetic endocrine disruptors like bisphenol A, are nonsteroidal substances with estrogenic activity.[7]

Pharmacology

Nonsteroidal estrogens act as agonists of the estrogen receptors, ERα and ERβ.


List of nonsteroidal estrogens

Synthetic

Pharmaceutical

SERMs like tamoxifen and raloxifene can also be considered to be nonsteroidal estrogens in some tissues.[8]

Environmental

Natural

See also

References

  1. ↑ 1.0 1.1 "Non-steroidal steroid receptor modulators". IDrugs 9 (7): 488–94. 2006. doi:10.2174/0929867053764671. PMID 16821162. 
  2. ↑ 2.0 2.1 "The nonsteroidal effects of diethylstilbestrol: the rationale for androgen deprivation therapy without estrogen deprivation in the treatment of prostate cancer". J. Urol. 170 (5): 1703–8. 2003. doi:10.1097/01.ju.0000077558.48257.3d. PMID 14532759. 
  3. ↑ "Diethylstilbestrol (DES) update: recommendations for the identification and management of DES-exposed individuals". J Midwifery Womens Health 48 (1): 19–29. 2003. doi:10.1016/s1526-9523(02)00370-7. PMID 12589302. 
  4. ↑ "Diethylstilbestrol exposure". Am Fam Physician 69 (10): 2395–400. 2004. PMID 15168959. 
  5. ↑ Philipp Y. Maximov; Russell E. McDaniel; V. Craig Jordan (23 July 2013). Tamoxifen: Pioneering Medicine in Breast Cancer. Springer Science & Business Media. pp. 4–. ISBN 978-3-0348-0664-0. https://books.google.com/books?id=p-W5BAAAQBAJ&pg=PA4. 
  6. ↑ Edward P. Gelmann; Charles L. Sawyers; Frank J. Rauscher, III (19 December 2013). Molecular Oncology. Cambridge University Press. pp. 885–. ISBN 978-0-521-87662-9. https://books.google.com/books?id=GrZEAgAAQBAJ&pg=PA885. 
  7. ↑ "Endocrine disruptors: can biological effects and environmental risks be predicted?". Regul. Toxicol. Pharmacol. 36 (1): 118–30. 2002. doi:10.1006/rtph.2002.1564. PMID 12383724. 
  8. ↑ V. Craig Jordan (2013). Estrogen Action, Selective Estrogen Receptor Modulators, and Women's Health: Progress and Promise. World Scientific. pp. 362–365. ISBN 978-1-84816-958-6. https://books.google.com/books?id=ejS6CgAAQBAJ&pg=PA362. 

Further reading



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