Selective estrogen receptor modulator

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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]


Overview

Selective estrogen receptor modulators (SERMs) are a class of medication that acts on the estrogen receptor.[1] A characteristic that distinguishes these substances from pure receptor agonists and antagonists is that their action is different in various tissues, thereby granting the possibility to selectively inhibit or stimulate estrogen-like action in various tissues.

Members

Members include:

Uses

SERMs are used dependent on their pattern of action in various tissues:

Some SERMs may be good replacements for hormone replacement therapy (HRT), which recent studies have called into question, although the above agents still have an unacceptably high risk of thrombosis and other side-effects to allow for widespread use.

Mechanism of action

Estrogenic compounds span a spectrum of activity ranging from:

  • full agonists (agonistic in all tissues) such as the natural endogenous hormone estrogen
  • mixed agonists/antagonistics (agonistic in some tissues while antagonist in others) such as tamoxifen (a SERM)
  • pure antagonists (antagonistic in all tissues) such as fulvestrant (ICI-182780).

The mechanism of mixed agonism/antagonism may differ depending on the chemical structure of the SERM, but for at least for some SERMs, it appears to be related to (1) the ratio of co-activator to co-repressor proteins in different cell types and (2) the conformation of the estrogen receptor induced by drug binding which in turn determines how strongly the drug/receptor complex recruits co-activators (resulting in an agonist response) relative to co-repressors (resulting in antagonism). For example, the prototypical SERM tamoxifen acts as an antagonist in breast and conversely an agonist in uterus. The concentration of steroid receptor co-activator 1 (SRC-1; NCOA1) is higher in uterus than in breast, therefore SERMs such as tamoxifen are more agonistic in uterus than in breast. In contrast, raloxifene behaves as an antagonist in both tissues. It appears that raloxifene more strongly recruits co-repressor proteins and consequently is still an antagonist in the uterus despite the higher concentration of co-activators relative to co-repressors.[2][3]

Actions

The actions of SERMs on various tissues:

References

  1. Riggs BL, Hartmann LC (2003). "Selective estrogen-receptor modulators -- mechanisms of action and application to clinical practice". N Engl J Med. 348 (7): 618–29. PMID 12584371. doi:10.1056/NEJMc030651. 
  2. Shang Y, Brown M (2002). "Molecular determinants for the tissue specificity of SERMs". Science. 295 (5564): 2465–8. PMID 11923541. doi:10.1126/science.1068537. 
  3. Smith CL, O'Malley BW (2004). "Coregulator function: a key to understanding tissue specificity of selective receptor modulators". Endocr Rev. 25 (1): 45–71. PMID 14769827. doi:10.1210/er.2003-0023. 

See also

Selective progesterone receptor modulator

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