G protein-coupled receptor (GPCR)

G protein-coupled receptors (GPCRs) are a large and diverse family of cell surface receptors that play a central role in transmitting signals from the extracellular environment into the cell. They are integral membrane proteins with seven transmembrane alpha helices. Upon ligand binding, GPCRs activate heterotrimeric G proteins, initiating intracellular signaling cascades that regulate numerous physiological processes. GPCRs are targets for a significant portion of modern medicinal drugs due to their ubiquity and involvement in essential biological processes.

Other names

7-transmembrane receptor7TM receptor

Modulation of GPCR activity via agonists, antagonists, or allosteric modulators, leading to altered downstream signaling cascades and cellular responses.