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Subject Categories: Review Article
British Journal of Pharmacology (2006) 147, S27–S37. doi:10.1038/sj.bjp.0706455
G-protein-coupled receptors: past, present and future
Stephen J Hill1
1Institute of Cell Signalling, University of Nottingham, Medical School, Queen's Medical Centre, Nottingham NG7 2UH
Correspondence: Stephen J. Hill, E-mail: stephen.hill@nottingham.ac.uk
Abstract
The G-protein-coupled receptor (GPCR) family represents the largest and most versatile group of cell surface receptors. Drugs active at these receptors have therapeutic actions across a wide range of human diseases ranging from allergic rhinitis to pain, hypertension and schizophrenia. This review provides a brief historical overview of the properties and signalling characteristics of this important family of receptors.
Keywords:
G-protein-coupled receptors, historical perspective, British Pharmacological Society 75th Anniversary, ligand binding, function, dimerization, cell signalling, desensitization
Abbreviations:
CGRP, calcitonin-gene-related peptide; CK1
, casein kinase 1; CRLR, calcitonin-receptor-like receptor; DADL, [D-Ala2,D-Leu5]enkephalin; DCI, dicholorisoprenaline; GFP, green fluorescent protein; GPCR, G-protein-coupled receptor; GRK, G-protein-coupled receptor kinase; ICI 174864, [N, N'-diallyl-Tyr1, Aib2,3]Leu5enkephalin; PKA, protein kinase A; PSD-95, postsynaptic density-95; RAMP, receptor-activity-modifying protein; SPAP, secreted placental alkaline phosphatase; TM, transmembrane
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