Mechanisms of regulation and function of G-protein-coupled receptor kinases

Figure 1 Schematic summary of the role of GRKs/arrestins in activation, signaling, and desensitization of GPCRs in the immune system. Agonist-activated GPCRs are phosphorylated rapidly by GRKs, leading to recruitment of arrestins. This process, called homologous desensitization, prevents further coupling of the receptor to its G protein, thereby reducing or preventing receptor signaling. In addition, GRKs and arrestins can also act as signal transducers in various signaling pathways. PLC: Phospholipase C.