Document Detail

Heterodimerization of g protein-coupled receptors: specificity and functional significance.
MedLine Citation:
PMID:  16109836     Owner:  NLM     Status:  MEDLINE    
G protein-coupled receptors (GPCRs) are cell surface receptors that mediate physiological responses to a diverse array of stimuli. GPCRs have traditionally been thought to act as monomers, but recent evidence suggests that GPCRs may form dimers (or higher-order oligomers) as part of their normal trafficking and function. In fact, certain GPCRs seem to have a strict requirement for heterodimerization to attain proper surface expression and functional activity. Even those GPCRs that do not absolutely require heterodimerization may still specifically associate with other GPCR subtypes, sometimes resulting in dramatic effects on receptor pharmacology, signaling, and/or internalization. Understanding the specificity and functional significance of GPCR heterodimerization is of tremendous clinical importance since GPCRs are the molecular targets for numerous therapeutic drugs.
Steven C Prinster; Chris Hague; Randy A Hall
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, P.H.S.; Review    
Journal Detail:
Title:  Pharmacological reviews     Volume:  57     ISSN:  0031-6997     ISO Abbreviation:  Pharmacol. Rev.     Publication Date:  2005 Sep 
Date Detail:
Created Date:  2005-08-19     Completed Date:  2005-10-28     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0421737     Medline TA:  Pharmacol Rev     Country:  United States    
Other Details:
Languages:  eng     Pagination:  289-98     Citation Subset:  IM    
Department of Pharmacology, Emory University School of Medicine, Atlanta, GA 30322, USA.
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MeSH Terms
Drug Design
Protein Transport
Receptors, G-Protein-Coupled / metabolism,  physiology*
Signal Transduction
Reg. No./Substance:
0/Ligands; 0/Receptors, G-Protein-Coupled

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