GRK 2 / ADRBK1 monoclonal antibody

Heterotrimeric G protein-mediated signal transduction is a dynamically regulated process with the intensity of signal decreasing over time despite the continued presence of the agonist. This phenomenon, referred to as agonistmediated desensitization, involves phosphorylation of the receptor by two classes of enzymes. The first are the second messenger-regulated kinases such as c-AMP dependent protein kinase A and protein kinase C. The second are the G protein-coupled receptor kinases (GRKs). At least seven members of the GRK family have been identified. These include rhodopsin kinase, GRK 1; two forms of β-adrenergic receptor kinase, GRK 2 (βARK, βARK1) and GRK 3 (βARK2); IT-11 (GRK 4); GRK 5, GRK 6 and GRK 7. Phosphorylation of receptors by GRKs appears to be strictly dependent on the receptor being in its agonist-activated state.