What does estrogen receptor alpha do?
The physiological functions of estrogenic compounds are modulated largely by the estrogen receptors subtypes alpha (ERα) and beta (ERβ). These proteins have actions in the cell nucleus, regulating transcription of specific target genes by binding to associated DNA regulatory sequences.
What drug is an estrogen receptor antagonist?
Tamoxifen is a nonsteroidal estrogen receptor antagonist that is mainly used for the treatment of estrogen receptor-positive breast cancer.
What are SERM drugs?
A: SERMs stands for “selective estrogen receptor modulators,” also called estrogen agonists/antagonists, which describes what these drugs do. They activate or block the estrogen receptors only in certain areas of the body and not others. That can make them safer than estrogen alone or result in fewer side effects.
What does the estrogen receptor beta do?
ERβ may inhibit cell proliferation and opposes the actions of ERα in reproductive tissue. ERβ may also have an important role in adaptive function of the lung during pregnancy. ERβ is a potent tumor suppressor and plays a crucial role in many cancer types such as prostate cancer and ovarian cancer.
Where is estrogen receptor alpha located?
The estrogen receptor alpha (ERα) is found predominately in the nucleus, both in hormone stimulated and untreated cells. Intracellular distribution of the ERα changes in the presence of agonists but the impact of different antiestrogens on the fate of ERα is a matter of debate.
What mean agonist?
Agonist: A substance that acts like another substance and therefore stimulates an action. Agonist is the opposite of antagonist. Antagonists and agonists are key players in the chemistry of the human body and in pharmacology.
What drugs are estrogen blockers?
Medications that stop the body from making estrogen after menopause
- Anastrozole (Arimidex). Anastrozole is used to reduce the risk of cancer recurrence in women who have been treated for early-stage breast cancer.
- Exemestane (Aromasin).
- Letrozole (Femara).
Which drugs are aromatase inhibitors?
Aromatase inhibitors stop the production of estrogen in postmenopausal women….There are three aromatase inhibitors:
- Arimidex (chemical name: anastrozole)
- Aromasin (chemical name: exemestane)
- Femara (chemical name: letrozole)
What are SERMs used for?
Selective estrogen receptor modulators (SERMs) are now being used as a treatment for breast cancer, osteoporosis and postmenopausal symptoms, as these drugs have features that can act as an estrogen agonist and an antagonist, depending on the target tissue.
What are the best SERMs?
Two of the most common SERMs are tamoxifen (Nolvadex, Soltamox) and raloxifene (Evista). There are several others as well, including lasofoxifene, bazedoxifene, and clomiphene citrate.
What is the role of estrogen receptor alpha ( ERα )?
Estrogen receptor alpha (ERα) plays a role in androgen independent PCas. Specifically, it has been suggested that ERα may provide alternate mechanism for PCa growth and progression by bypassing androgen signaling.
Are there any estrogen receptor antagonists for breast cancer?
In light of above, in the present review we have covered the role of estrogen receptor α antagonists as anticancer agents against breast cancer especially over the past decade as there was no such extensive report is found in the literature.
How are estrogen antagonists different from estrogen agonists?
CoRs inhibit transcription. The SERMs are partial agonists, antagonizing the effects of estrogen in some tissues (breast) and stimulating estrogen receptors in others (bone, brain, liver). This is in contrast to the estrogen antagonists (e.g., clomiphene), which block estrogen receptors in all tissues.
How does an estrogen receptor antagonist ( SERM ) work?
Estrogen receptor antagonists inhibit transcription by promoting the binding of co-repressors (CoRs) to the ERE. CoRs inhibit transcription. The SERMs are partial agonists, antagonizing the effects of estrogen in some tissues (breast) and stimulating estrogen receptors in others (bone, brain, liver).