G Protein-Coupled Receptors: Dynamic Machines for Signaling Pain and Itch

G protein-coupled receptors (GPCRs) are the major class of sensory proteins and a primary therapeutic target in the pathways to pain and itch. GPCRs are complex signaling machines. Their association with ligands, other receptors, and signaling and regulatory partners induces GPCRs to adopt distinct...

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Bibliographic Details
Published in:Neuron (Cambridge, Mass.) Mass.), 2015-11, Vol.88 (4), p.635-649
Main Authors: Geppetti, Pierangelo, Veldhuis, Nicholas A., Lieu, TinaMarie, Bunnett, Nigel W.
Format: Article
Language:English
Subjects:
Animals
Binding sites
Humans
Inflammation
Laboratories
Ligands
Narcotics
Neurons
Nociceptors - metabolism
Nociceptors - physiology
Pain
Pain - metabolism
Physiology
Proteins
Pruritus - metabolism
Receptors, G-Protein-Coupled - metabolism
Receptors, G-Protein-Coupled - physiology
Sensory Receptor Cells - metabolism
Sensory Receptor Cells - physiology
Signal Transduction
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Summary:G protein-coupled receptors (GPCRs) are the major class of sensory proteins and a primary therapeutic target in the pathways to pain and itch. GPCRs are complex signaling machines. Their association with ligands, other receptors, and signaling and regulatory partners induces GPCRs to adopt distinct conformations and to traffic to microdomains within plasma and endosomal membranes. This conformational and positional dynamism controls GPCR signaling in time and space and defines the outcome of receptor activation. An understanding of the dynamic nature of GPCRs within primary sensory neurons and neighboring cells brings new insights into their contributions to the physiology and pathophysiology of pain and itch and provides novel opportunities for therapeutic intervention. G protein-coupled receptors are the major class of sensory proteins and an important therapeutic target in the pathways to pain and itch. Herein, Geppetti and colleagues discuss how alterations in the conformation and trafficking of these proteins influence sensory transduction.
ISSN:0896-6273
1097-4199
DOI:10.1016/j.neuron.2015.11.001