title: G Protein-Coupled Receptors: Dynamic Machines for Signaling Pain and Itch.
abstract: 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.
authors.affiliation: Department of Health Sciences, Clinical Pharmacology Unit, University of Florence, 6-50139, Florence, Italy.
authors.forename: Pierangelo
authors.initials: P
authors.lastname: Geppetti
authors.affiliation: Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, VIC 3052, Australia; Australian Research Council, Centre of Excellence in Convergent Bio-Nano Science and Technology, Monash University, 381 Royal Parade, Parkville, VIC 3052, Australia.
authors.forename: Nicholas A
authors.initials: NA
authors.lastname: Veldhuis
authors.affiliation: Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, VIC 3052, Australia; Australian Research Council, Centre of Excellence in Convergent Bio-Nano Science and Technology, Monash University, 381 Royal Parade, Parkville, VIC 3052, Australia.
authors.forename: TinaMarie
authors.initials: T
authors.lastname: Lieu
authors.affiliation: Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, VIC 3052, Australia; Australian Research Council, Centre of Excellence in Convergent Bio-Nano Science and Technology, Monash University, 381 Royal Parade, Parkville, VIC 3052, Australia; Department of Pharmacology and Therapeutics, University of Melbourne, Melbourne,VIC 3010, Australia. Electronic address: nigel.bunnett@monash.edu.
authors.forename: Nigel W
authors.initials: NW
authors.lastname: Bunnett
mesh_terms: D000818:Animals; D006801:Humans; D009619:Nociceptors / Q000378:metabolism* / Q000502:physiology; D010146:Pain / Q000378:metabolism*; D011537:Pruritus / Q000378:metabolism; D043562:Receptors, G-Protein-Coupled / Q000378:metabolism* / Q000502:physiology; D011984:Sensory Receptor Cells / Q000378:metabolism / Q000502:physiology; D015398:Signal Transduction
chemical_list: D043562:Receptors, G-Protein-Coupled