logo
AAT Bioquest

How are G-protein linked receptors activated?

Posted March 21, 2024


Answer

G-protein linked receptors (GPCRs) are activated when a specific ligand, such as a hormone or neurotransmitter, binds to the extracellular region of the receptor protein. This binding event induces a conformational change in the receptor, which triggers the activation of an associated heterotrimeric G protein. The G protein consists of two parts: an alpha subunit and beta-gamma subunits. The activated alpha subunit can interact with and regulate the activity of various effector proteins (such as adenylyl cyclase or phospholipase C) depending on the specific type of G protein involved. These effector proteins generate second messenger molecules, such as cyclic AMP (cAMP) or inositol trisphosphate (IP3), which propagate the signal within the cell. 

Additional resources

GPCRs in Intracellular Compartments: New Targets for Drug Discovery

G-Protein-Coupled Receptors (GPCR)

Cell Meter™ Beta-Arrestin Translocation GPCR Signaling Kit