G Protein–Coupled Receptor Oligomerization: Implications for G Protein Activation and Cell Signaling

ABSTRACT—The cardiovascular system is richly endowed with G protein–coupled receptors (GPCRs), members of the largest family of plasma membrane-localized receptors. During the last 10 years, it has become increasingly clear that many, if not all, GPCRs function in oligomeric complexes, as either hom...

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Bibliographic Details
Published inCirculation research Vol. 94; no. 1; pp. 17 - 27
Main Author Breitwieser, Gerda E
Format Journal Article
LanguageEnglish
Published Hagerstown, MD American Heart Association, Inc 09.01.2004
Lippincott
Lippincott Williams & Wilkins Ovid Technologies
Subjects
Animals
Biological and medical sciences
Cardiovascular System - metabolism
Dimerization
Fundamental and applied biological sciences. Psychology
Heterotrimeric GTP-Binding Proteins - metabolism
Humans
Models, Biological
Receptors, G-Protein-Coupled - metabolism
Signal Transduction
Vertebrates: cardiovascular system
Signal transduction
Vertebrata
Mammalia
G protein-coupled receptors
oligomerization
heterodimerization
G protein activation
Activation
Receptor protein
Circulatory system
G protein
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Summary:ABSTRACT—The cardiovascular system is richly endowed with G protein–coupled receptors (GPCRs), members of the largest family of plasma membrane-localized receptors. During the last 10 years, it has become increasingly clear that many, if not all, GPCRs function in oligomeric complexes, as either homo- or hetero-oligomers. This review explores the mechanistic implications of GPCR dimerization and/or oligomerization on receptor activation and interactions with G proteins. The effects of GPCR oligomerization on receptor pharmacology, GPCR-mediated signaling, and potential contributions to GPCR crosstalk will be considered in the context of receptors important in the cardiovascular system. Our evolving understanding of the structural and functional consequences of GPCR oligomerization may provide novel and more selective sites for pharmacological tuning of cardiovascular function.
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
ObjectType-Feature-3
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ObjectType-Review-1
ISSN:0009-7330
1524-4571
DOI:10.1161/01.RES.0000110420.68526.19