GPCR Membrane Preparations

Background of GPCR

G-protein-coupled receptors (GPCRs) mediate the majority of our physiological reactions to hormones, neurotransmitters, and environmental stimulants, and hence offer a wide range of therapeutic possibilities. All GPCRs are characterized by the presence of seven membrane-spanning -helical segments separated by alternating intracellular and extracellular loop sections at the most basic level. GPCRs have a unique set of signaling activities encompassing various G-protein subtypes, as well as G-protein-independent signaling pathways and intricate regulation processes.

Application of GPCR Membrane Preparations

Drug development has been transformed by the introduction of membrane ligand binding assays and high-throughput screening. Ligand binding assays allow us to see how a ligand or a new synthetic molecule interacts with a target protein and assess affinity and kinetics of those interactions, while HTS helps to automate research and shorten development time. Cell signaling and ligand binding in GPCRs are controlled by changes in the cell membrane and the membrane itself.