Selective estrogen receptor modulators (SERMs) is a class of medication that acts on the estrogen receptor. A characteristic that distinguishes these substances from receptor agonists and antagonists is that their action is different for various tissues, thereby granting the possibility to selectively inhibit or stimulate estrogen-like action in various tissues.
Members
Members are:
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 has recently been discredited, although the above agents still have an unacceptably high risk of thrombosis and other side-effects to allow for widespread use.
Method of action
Although the SERMs have no immediate structural relationship with 17β-estradiol, they are stereochemically similar to this estrogen.
There are three types of estrogen receptors, which are intracellular : α (α homodimer), β (β homodimer) and the heterodimer (α- and β-receptor heterodimers):. Different tissues have more or less of each class. In turn, each SERM has more affinity to one and less to the other estrogen receptor isoform. The α-receptor is generally stimulatory, but the β-receptor may inhibit the α-isoform as well as suppressing transcription independently.
Genes activated or suppressed by estrogen receptors generally have an estrogen response element sequence in their promotor.
Some SERMs, through this process, also augment the transcription of coactivator molecules, which may be indispensable for their pharmacological action.
Actions
The actions of SERMs on various tissues:
References
- Riggs BL, Hartmann LC. Selective estrogen-receptor modulators - mechanisms of action and application to clinical practice. N Engl J Med 2003;348:618-29. PMID 12584371.
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