Fulvestrant
Estrogen receptor antagonist / A 17β-estradiol analog that acts as an estrogen receptor (ER) antagonist and GPR30/GPER agonist with high binding affinity.1,2 First-in-class SERD (selective ER degrader) because it inhibits ER transcriptional activity and leads to its degradation.3 Exhibits mixed neuroprotective activity in vivo.4 Clinically useful option for some advanced breast cancers.5
Biochemicals & reagents
129453-61-8
ICI-182,780; ZD-9238
Osborne et al. (2004), Fulvestrant: an oestrogen receptor antagonist with a novel mechanism of action; Br. J. Cancer 90 (Suppl 1):S2 Thomas et al. (2005), Identity of an estrogen membrane receptor coupled to a G protein in human breast cancer cells; Endocrinology 146 624 Wardley (2002), Fulvestrant: a review of its development, pre-clinical and clinical data; Int. J. Clin. Pract. 56 305 Castro et al. (2012), Coumestrol has neuroprotective effects before and after cerebral ischemia in female rats; Brain Res. 1474 82 Blackburn et al. (2018), Fulvestrant for the treatment of advanced breast cancer; Expert Rev. Anticancer Ther. 18 619
-20°C
TARGET: Transcription factor; Molecular glue -- PATHWAY: Estrogen; Transcription -- RESEARCH AREA: Neuroscience -- DISEASE AREA: Cancer; NeurodegenerationIschemia