G protein-coupled receptors (GPCR) are so named because of their regulation of an intracellular heterotrimeric complex made up of G alpha, and G beta gamma subunits. Ligand binding to receptor stimulates the well-described exchange of GDP for GTP by G alpha. This activity lies at the apex of numerous signaling cascades induced by a range of different stimuli including light, odorants, amino acids, nucleotides, lipids, and peptides/proteins. GPCRs make up the largest family of integral membrane proteins and account for approximately 5% of all genes found in the human genome. Clinically, approximately 45% of modern drugs target GPCRs, underscoring the importance of having quality research tools to study their functions.

R&D Systems continues to expand its selection of products for GPCR research to include reagents for at least 20 chemokine receptors, as well as other GPCRs in key areas of biological science.