Development of a Generic Dual-Reporter Gene Assay for Screening G-Protein-Coupled Receptors

Development of generic calcium imaging assay for monitoring Gi-coupled receptors and G-protein interaction.

G-protein-coupled receptors (GPCRs) are important therapeutic targets for many areas of drug research and development. Although chimeric Galpha16 proteins are valuable tools for detecting the activation of Galpha(i/o)-coupled receptors, the details of the activation process remain unclear. The authors introduce a series of chimeras that combine both Galpha16 and Galpha(i/o) (Galpha(16/o), Galph...

Assay and array technologies for G-protein coupled receptors

This paper describes a novel strategy to create a microarray of G-protein Coupled Receptors (GPCRs), an important group of membrane proteins both physiologically and pharmacologically. The H1-histamine receptor and the M2-muscarinic receptor were both used as model GPCRs in this study. The receptor proteins were embedded in liposomes created from the cellular membrane extracts of Spodoptera fru...

G Protein-coupled receptors

G protein-coupled receptors and heterotrimeric G proteins can diffuse laterally in the plasma membrane such that one receptor can catalyze the activation (GDP/GTP exchange) of multiple G proteins. In some cases, these processes are fast enough to support molecular signal amplification, where a single receptor maintains the activation of multiple G proteins at steady-state. Amplification in cell...

G-protein-coupled receptors.

G-Protein-coupled receptors mediate many of the hypnotic and analgesic actions of the drugs employed in anesthesia. Notably, opioid agonists represent the most successful and efficacious class of analgesic agents employed over the last century. Also, major clinical advances have been made by the study of alpha(2) adrenoceptor agonists, which possess both hypnotic and analgesic qualities that ar...

Modelling G protein-coupled receptors