Estriol (Oestriol)

Description: Estriol (also called NSC-12169; Oestriol) is a potent antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells. Estriol’s efficacy is due to the interference between estradiol-induced positive cooperative binding and receptor dimerization, as well as the binding of hER complexes to ERE. MTT assays using G-1 shows that, in SkBr3 cells, the proliferative effect induced by 100 nM G-1 is abolished in the presence of 1 uM estriol which acts as an antagonist of GPR30-dependent pathway.

References: Mol Cell Endocrinol. 2010 May 14; 320(1-2):162-70; Lab Invest. 2006 Mar; 86(3):286-96.