Regulated GPCR trafficking to the plasma membrane: general issues and the CCR5 chemokine receptor example.

The regulated export of nascent G protein coupled receptors (GPCRs) from intracellular stores is an emerging concept with important implications in cell biology and pharmacology. This phenomenon requires a complex network of interactions between GPCRs with either chaperones and escort proteins or gatekeepers, which are respectively involved in the progression of GPCRs along the biosynthetic pathway to the plasma membrane or in their retention in intracellular compartments. The regulated export of GPCRs is also controlled by external stimuli and might represent an adaptive mechanism to specific physiological constraints, such as the sustained activation of the CCR5 chemokine receptor in the context of chemotaxis.