Abstract 2847 Cryo-EM analysis of the GRK2-GPCR complex

G-protein coupled receptors (GPCRs) are the most functionally diverse classes of membrane receptors. G protein-coupled receptor kinases (GRKs) act as 'brakes' to terminate GPCR signaling by recruiting arrestins, leading to receptor internalization. Consequently, aberrant GRK expression and activity disrupts cellular homeostasis by prematurely terminating or failing to terminate GPCR signaling, thus greatly impacting cellular responses. GRK2, abundantly expressed in the cardiovascular tissue, is an important regulator of β-adrenergic receptors (β-ARs).