What does tamoxifen do to cells?
Tamoxifen attaches to the hormone receptors in the cancer cell, blocking estrogen from attaching to the receptors. This slows or stops the growth of the tumor by preventing the cancer cells from getting the hormones they need to grow.
How does tamoxifen work on a cellular level?
Drug-resistant cells sequester weak base chemotherapeutics in acidic organelles away from their sites of action in the cytosol and nucleus. This work reports that tamoxifen causes redistribution of weak base chemotherapeutics from acidic organelles to the nucleus in drug-resistant cells.
What is the mechanism of action of tamoxifen?
Tamoxifen (TAM) is known to have a dual mechanism of action: (1) to compete with 17β-estradiol (E2) at the receptor site and to block the promotional role of E2 in breast cancer; and (2) to bind DNA after metabolic activation and to initiate carcinogenesis.
What receptors does tamoxifen block?
The drug tamoxifen rescinds this permission by block- ing the reception of the estrogen message. Tamoxifen binds to the estrogen receptor but does not activate it fully, halting estrogen-induced growth. Of course, estrogen has many effects throughout the body. It is dangerous to block its action indiscriminately.
What is the chemical formula for tamoxifen?
Tamoxifen | C26H29NO – PubChem.
Is tamoxifen an immunosuppressant?
People considered more at risk include those having: Chemotherapy. Immunotherapy or targeted (biological) therapies such as trastuzumab emtansine (Kadcyla) or everolimus (Afinitor)
Does tamoxifen cause apoptosis?
Tamoxifen is composed of a triphenylethylene backbone structure and functions by combining with ERα (6) and inhibiting the estradiol (E2)-ER genetic pathway, which inhibit proliferation and induce apoptosis in breast cancer cells.
What is the chemical structure of tamoxifen?
Is tamoxifen an agonist or 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.
Is tamoxifen a protein kinase inhibitor?
In addition to its activity as a SERM, tamoxifen is a potent and selective protein kinase C inhibitor, and is active in this regard at therapeutic concentrations. This action is thought to underlie the efficacy of tamoxifen in the treatment of bipolar disorder. Tamoxifen is an inhibitor of P-glycoprotein.
What functional groups are in tamoxifen?
Analogs were generated by modification of the hydrophilic functional group of Tamoxifen by hydroxyl, amide, carboxyl, and sulfhydryl functional groups, in an attempt to improve their activity and selectivity.
Can tamoxifen be compounded?
The selective estrogen receptor modulator, tamoxifen, effectively slows the progression of estrogen-positive breast cancer and reduces the possibility of this cancer developing in women at high risk….CHEBI:41774.
| Synonyms | Sources |
|---|---|
| Tamoxifen | KEGG COMPOUND |
| trans-Tamoxifen | ChemIDplus |