Competitive Binding Assay for the G-Protein-Coupled Receptor 30 (GPR30) or G-Protein-Coupled Estrogen Receptor (GPER).
Thomas Thekkumkara, Russell Snyder, Vardan T Karamyan
Author Information
Thomas Thekkumkara: Department of Biomedical Sciences, Texas Tech University Health Sciences Center, 1300 Coulter Drive, Amarillo, TX, 79106, USA. thomas.thekkumkara@ttuhsc.edu.
Russell Snyder: Department of Biomedical Sciences, Texas Tech University Health Sciences Center, 1300 Coulter Drive, Amarillo, TX, 79106, USA.
Vardan T Karamyan: Department of Pharmaceutical Sciences, Texas Tech University Health Sciences Center, 1300 South Coulter, Amarillo, TX, 79106, USA.
The role of 2-methoxyestradiol is becoming a major area of investigation because of its therapeutic utility, though its mechanism is not fully explored. Recent studies have identified the G-protein-coupled receptor 30 (GPR30, GPER) as a high-affinity membrane receptor for 2-methoxyestradiol. However, studies aimed at establishing the binding affinities of steroid compounds for specific targets are difficult, as the tracers are highly lipophilic and often result in nonspecific binding in lipid-rich membrane preparations with low-level target receptor expression. 2-Methoxyestradiol binding studies are essential to elucidate the underlying effects of this novel estrogen metabolite and to validate its targets; therefore, this competitive receptor-binding assay protocol was developed in order to assess the membrane receptor binding and affinity of 2-methyoxyestradiol.
