Document Detail

Theme and variations on kinetics of GPCR activation/deactivation.
MedLine Citation:
PMID:  20836728     Owner:  NLM     Status:  MEDLINE    
G protein-coupled receptors (GPCRs) initiate intracellular signaling pathways in response to physiologically and medically important extracellular ligands such as peptide and large glycoprotein hormones, neurotransmitters, sensory stimuli (odorant and taste molecules, light), calcium, l-amino acids, and are the target of many clinical drugs. The conversion of these extracellular stimuli into intracellular signals involves sequential and reversible reactions that initially take place at the plasma membrane. These reactions are mediated not only by dynamic interactions between ligands, receptors and heterotrimeric G proteins, but also by conformational changes associated with the activation/deactivation process of each protein. This review discusses the kinetic characteristics and rate-limiting reactions engaged in signal propagation that are involved in systems as diverse as neurotransmitter and hormonal signaling, and that have been recorded in live cells by Förster resonance energy transfer (FRET) approaches.
Jean-Pierre Vilardaga
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Review    
Journal Detail:
Title:  Journal of receptor and signal transduction research     Volume:  30     ISSN:  1532-4281     ISO Abbreviation:  J. Recept. Signal Transduct. Res.     Publication Date:  2010 Oct 
Date Detail:
Created Date:  2010-09-22     Completed Date:  2011-01-13     Revised Date:  2014-09-15    
Medline Journal Info:
Nlm Unique ID:  9509432     Medline TA:  J Recept Signal Transduct Res     Country:  England    
Other Details:
Languages:  eng     Pagination:  304-12     Citation Subset:  IM    
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MeSH Terms
Adrenergic Agonists / chemistry,  metabolism
Cell Membrane / metabolism*
Fluorescence Resonance Energy Transfer
Models, Molecular
Molecular Structure
Protein Conformation
Receptors, G-Protein-Coupled* / chemistry,  metabolism
Signal Transduction / physiology*
Grant Support
Reg. No./Substance:
0/Adrenergic Agonists; 0/Receptors, G-Protein-Coupled

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