PhytoSERM are botanically derived substances that possess SERM qualities, similar to synthetically manufactured drugs of the same category.

Mechanism of action

Similarly to SERMs, phyto-SERMs act on the estrogen receptor

Estrogen receptor

Estrogen receptor refers to a group of receptors that are activated by the hormone 17β-estradiol . Two types of estrogen receptor exist: ER, which is a member of the nuclear hormone family of intracellular receptors, and the estrogen G protein-coupled receptor GPR30 , which is a G protein-coupled...

 in a selective manner, either as agonist

Agonist

An agonist is a chemical that binds to a receptor of a cell and triggers a response by that cell. Agonists often mimic the action of a naturally occurring substance...

s, or as antagonist

Receptor antagonist

A receptor antagonist is a type of receptor ligand or drug that does not provoke a biological response itself upon binding to a receptor, but blocks or dampens agonist-mediated responses...

s, thereby granting the possibility to selectively stimulate or inhibit estrogen-like responses in different tissues. The molecular basis for this discrimination lies in the variability of transcription coregulator

Transcription coregulator

In molecular biology and genetics, transcription coregulators are proteins that interact with transcription factors to either activate or repress the transcription of specific genes. Transcription coregulators that activate gene transcription are referred to as coactivators while those that...

s in different tissues which interact with the estrogen receptor. Furthermore many phytoestrogen (including phyto-SERMs) appear to be somewhat selective in binding for the estrogen receptor beta

Estrogen receptor beta

Estrogen receptor beta , also known as NR3A2 , is a nuclear receptor which is activated by the sex hormone estrogen. In humans, ER-β is encoded by the ESR2 gene.- Function :...

 (ERβ) compared to the estrogen receptor alpha

Estrogen receptor alpha

Estrogen receptor alpha , also known as NR3A1 , is a nuclear receptor that is activated by the sex hormone estrogen...

 (ERα) paralog. These two forms of the estrogen receptor display somewhat different tissue distributions and regulate a partially-overlapping set of genes.

PhytoSERMs' unique mechanism of action, being able to target specific tissues precisely while unaffecting others, may make them safer candidates for treatment of estrogen deficiencies.

Category members

• Femarelle (DT56a)
  Femarelle (DT56a)
  Femarelle is as a selective estrogen receptor modulator for the treatment of menopause and bone health. DT56a is a standardized compound derived from soybean.-Mode of Action:...
  
   - a phytoSERM used for the treatment of menopause symptoms and bone health

Indications

PhytoSERMs are suitable for treating estrogen deficiencies that cause menopause symptoms, osteopenia and osteoporosis.

See also

• Selective estrogen receptor modulator
  Selective estrogen receptor modulator
  Selective Estrogen Receptor Modulators are a class of compounds that act on the estrogen receptor. 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...
  
  
• Femarelle (DT56a)
  Femarelle (DT56a)
  Femarelle is as a selective estrogen receptor modulator for the treatment of menopause and bone health. DT56a is a standardized compound derived from soybean.-Mode of Action:...
  
  , Femarelle web site
• Phytoestrogen