Figure 3.
(A) Receptor deactivation is mediated by the RGS family of proteins. RGS alters the conformation of Gα-GTP complex making it a better hydrolase, which accelerates the hydrolysis of GTP to GDP. (B) GPCR desensitization through internalization occurs when GRK phosphorylates the activated receptor promoting β-arresting binding, which sterically hinders receptor-G protein interaction. The receptor is either degraded or recycled back to the cell surface. Figure 3A was adapted from Neubig, et al. [191] and 3B was adapted from Pierce, et al. [4].