Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding.

ABSTRACT: G-Protein-Coupled Receptors (GPCRs) are a large family of transmembrane receptors that play critical roles in normal cellular physiology and constitute a major pharmacological target for multiple indications, including analgesia, blood pressure regulation, and the treatment of psychiatric disease. Upon ligand binding, GPCRs catalyze the activation of intracellular G-proteins by stimulating the incorporation of guanosine triphosphate (GTP). Activated G-proteins then stimulate signaling pathways that elicit cellular responses. GPCR signaling can be monitored by measuring the incorporation of a radiolabeled and non-hydrolyzable form of GTP, [³⁵S]guanosine-5'-O-(3-thio)triphosphate ([³⁵S]GTPγS), into G-proteins. Unlike other methods that assess more downstream signaling p

SUBMITTER: Vasavda C 

PROVIDER: S-EPMC5608332 | biostudies-literature | 2017 Jun

REPOSITORIES: biostudies-literature