ERRγ inverse agonist 1,2316832

Measurement of Agonist-Stimulated [35S]GTPγS Binding to Assess Total G-Protein and Gα-Subtype-Specific Activation by G-Protein-Coupled Receptors

preparations, GTP can be substituted by 35 S-labeled guanosine 5′-O -(3-thio)triphosphate ([35 S]GTγS) and on agonist stimulation a stable [35 S]GTPγS-Gα complex will form and accumulate. Separation of 35 S-bound GTPγS-Gα complexes from free [35 S]GTPγS allows

Measurement of Agonist-Stimulated [35S]GTPS Binding to Cell Membranes

This chapter describes a functional assay which measures the increase in guanine nucleotide exchange at G-proteins in cell membranes, resulting from agonist binding to G-protein-coupled receptors (GPCRs), by monitoring the binding of [35 S

In Vitro Assays of Rod and Cone Opsin Activity: Retinoid Analogs as Agonists and Inverse Agonists

transduction cascade. The native ligand, 11-cis- retinal, acts as an inverse agonist to both the apoproteins of rod and cone visual pigments (opsins); all-trans- retinal is an agonist. Truncated analogs of retinal have been used to characterize structure–