G Protein-Coupled Receptor Resensitization Paradigms.

G Protein-Coupled Receptor Resensitization Paradigms. Int Rev Cell Mol Biol. 2018;339:63-91 Authors: Gupta MK, Mohan ML, Naga Prasad SV Abstract Cellular responses to extracellular milieu/environment are driven by cell surface receptors that transmit the signal into the cells resulting in a synchronized and measured response. The ability to provide such exquisite responses to changes in external environment is mediated by the tight and yet, deliberate regulation of cell surface receptor function. In this regard, the seven transmembrane G protein-coupled receptors (GPCRs) are the largest family of cell surface receptors that regulate responses like cardiac contractility, vision, and olfaction including platelet activation. GPCRs regulate these plethora of events through GPCR-activation, -desensitization, and -resensitization. External stimuli (ligands or agonists) activate GPCR initiating downstream signals. The activated GPCR undergoes inactivation or desensitization by phosphorylation and binding of β-arrestin resulting in diminution of downstream signals. The desensitized GPCRs are internalized into endosomes, wherein they undergo dephosphorylation or resensitization by protein phosphatase to be recycled back to the cell membrane as naïve GPCR ready for the next wave of stimuli. Despite the knowledge that activation, desensitization, and resensitization shoulder an equal role in maintaining GPCR function, major advances have been...
Source: International Review of Cell and Molecular Biology - Category: Cytology Authors: Tags: Int Rev Cell Mol Biol Source Type: research