Tamoxifen citrate
ER antagonist; GPR30 agonist / Estrogen receptor antagonist/partial agonist. Induces oxidative stress and apoptosis in estrogen receptor-negative cancer cell lines1. Displays neuroprotective effects in permanent focal ischemia2. Inhibits PKC3. Potent agonist at GPR30 (membrane estrogen receptor)4. Clinically useful breast cancer agent5.
Biochemicals & reagents
54965-24-1
ICI-46474
1) Ferlini et al. (1999), Tamoxifen induces oxidative stress and apoptosis in oestrogen receptor-negative human cancer cell lines; Br. J. Cancer, 79 257 2) Kimelberg et al. (2003), Neuroprotective activity of tamoxifen in permanent focal ischemia; J. Neurosurg., 99 138 3) Couldwell et al. (1994), Protein kinase C inhibitors induce apoptosis in human malignant glioma cell lines FEBS Lett., 345 43 4) Thomas et al. (2005), Identity of an estrogen membrane receptor coupled to a G protein in human breast cancer cells; Endocrinology, 146 624 5) Jordan et al. (2006), Tamoxifen (ICI46,474) as a targeted therapy to treat and prevent breast cancer; Br. J. Pharmacol., 147 S269
RT
TARGET: Transcription factor; GPCR; Cytochrome/MDR -- PATHWAY: Estrogen; Apoptosis inducer; Autophagy; Transcription -- RESEARCH AREA: Neuroscience; Oxidative stress; Cell death -- DISEASE AREA: Cancer; Ischemia