Which acts an estrogen receptor agonist?
Resveratrol acts as an estrogen receptor (ER) agonist in breast cancer cells stably transfected with ER alpha. Int J Cancer.
How does an antagonist bind to estrogen receptor?
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).
Is tamoxifen an antagonist?
Tamoxifen is both an antagonist and an agonist of the estrogen receptor. However, a molecular explanation exists for this apparent paradox. The dual action is a function of the estrogen receptor complex present in a particular cell or tissue.
What drug is an estrogen receptor antagonist?
Fulvestrant: a new type of estrogen receptor antagonist for the treatment of advanced breast cancer. Drugs Today (Barc).
What are agonist drugs?
Listen to pronunciation. (A-guh-nist) A drug or substance that binds to a receptor inside a cell or on its surface and causes the same action as the substance that normally binds to the receptor.
What is an example of an agonist drug?
An agonist is a drug that activates certain receptors in the brain. Full agonist opioids activate the opioid receptors in the brain fully resulting in the full opioid effect. Examples of full agonists are heroin, oxycodone, methadone, hydrocodone, morphine, opium and others.
Why is tamoxifen an agonist?
If a cell type requires activating factors 1 and 2 of the estrogen receptor to be functioning concurrently, tamoxifen is antagonistic. However, if a cell or tissue requires only activating factor 1 to interact with transcription factors at the promoter, tamoxifen is agonistic.
What type of drug is tamoxifen?
Tamoxifen is in a class of medications known as antiestrogens. It blocks the activity of estrogen (a female hormone) in the breast. This may stop the growth of some breast tumors that need estrogen to grow.
Is tamoxifen an agonist or antagonist?
Which drugs are aromatase inhibitors?
- Anastrozole (Arimidex)
- Exemestane (Aromasin)
- Letrozole (Femara)
What is the pharmacology of alpha adrenergic agonists?
General Pharmacology. Alpha-adrenoceptor agonists (α-agonists) bind to α-receptors on vascular smooth muscle and induce smooth contraction and vasoconstriction, thus mimicking the effects of sympathetic adrenergic nerve activation to the blood vessels. Vascular smooth muscle has two types of alpha-adrenoceptors: alpha1 (α1) and alpha2 (α2).
Are ERβ-selective agonists therapeutic?
From a clinical perspective, ERβ-selective agonists might be therapeutically useful for some types of cancer, hot flashes and several other inflammatory diseases.
What are the alpha-1 and alpha-2 agonists?
Alpha-1 agonists: metaraminol, methoxamine, ozymetazoline, phenylephrine. Alpha-1 antagonist: doxazosin, prazosin, tamsulosin, terazosin. Alpha-2 agonists: brimonidine, clonidine, dexmedetomidine, guanabenz, guanfacine. Alpha-2 antagonist: idazoxan, RX821002, yohimibine, rauwolscine.
What is estrogen receptor alpha (ERα)?
From Wikipedia, the free encyclopedia Estrogen receptor alpha (ERα), also known as NR3A1 (nuclear receptor subfamily 3, group A, member 1), is one of two main types of estrogen receptor, a nuclear receptor that is activated by the sex hormone estrogen. In humans, ERα is encoded by the gene ESR1 (EStrogen Receptor 1).