G protein-coupled receptor binding

Definition

Target type: molecularfunction

Binding to a G protein-coupled receptor. [GOC:ceb, GOC:dph]

G protein-coupled receptor (GPCR) binding is a fundamental process in cellular signaling, mediating a wide range of physiological responses. GPCRs are transmembrane proteins that act as receptors for diverse extracellular stimuli, including hormones, neurotransmitters, light, and odorants. When a ligand binds to its cognate GPCR, it triggers a conformational change in the receptor, activating its intracellular signaling cascade. This activation typically involves the interaction of the GPCR with a heterotrimeric G protein, a complex composed of alpha, beta, and gamma subunits. Upon ligand binding, the GPCR catalyzes the exchange of GDP for GTP on the alpha subunit of the G protein. This GTP-bound alpha subunit dissociates from the beta-gamma dimer and interacts with downstream effector molecules, such as adenylyl cyclase or phospholipase C, to modulate intracellular signaling pathways. The activated effector molecules produce second messengers, such as cAMP or diacylglycerol, which further amplify the signal and lead to changes in cellular functions. The GPCR-mediated signaling cascade is tightly regulated by various mechanisms, including receptor desensitization, phosphorylation, and internalization. This dynamic regulation ensures that the cellular response to ligand binding is appropriate and transient. In summary, GPCR binding initiates a complex signaling cascade that involves conformational changes in the receptor, G protein activation, downstream effector molecule activation, second messenger production, and ultimately, alteration of cellular processes.'
"

Proteins (14)

Compounds (378)