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rdf:type | |
lifeskim:mentions | |
pubmed:dateCreated |
1998-11-30
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pubmed:abstractText |
G protein-coupled receptor kinases (GRKs) constitute a family of six mammalian serine/threonine protein kinases that phosphorylate agonist-bound, or activated, G protein-coupled receptors (GPCRs) as their primary substrates. GRK-mediated receptor phosphorylation rapidly initiates profound impairment of receptor signaling, or desensitization. This review focuses on the regulation of GRK activity by a variety of allosteric and other factors: agonist-stimulated GPCRs, beta gamma subunits of heterotrimeric GTP-binding proteins, phospholipid cofactors, the calcium-binding proteins calmodulin and recoverin, posttranslational isoprenylation and palmitoylation, autophosphorylation, and protein kinase C-mediated GRK phosphorylation. Studies employing recombinant, purified proteins, cell culture, and transgenic animal models attest to the general importance of GRKs in regulating a vast array of GPCRs both in vitro and in vivo.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:issn |
0066-4154
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
67
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
653-92
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pubmed:dateRevised |
2007-11-15
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pubmed:meshHeading |
pubmed-meshheading:9759500-Allosteric Regulation,
pubmed-meshheading:9759500-Animals,
pubmed-meshheading:9759500-Disease,
pubmed-meshheading:9759500-GTP-Binding Proteins,
pubmed-meshheading:9759500-Humans,
pubmed-meshheading:9759500-Mammals,
pubmed-meshheading:9759500-Protein-Serine-Threonine Kinases,
pubmed-meshheading:9759500-Receptors, Cell Surface,
pubmed-meshheading:9759500-Signal Transduction,
pubmed-meshheading:9759500-Substrate Specificity
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pubmed:year |
1998
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pubmed:articleTitle |
G protein-coupled receptor kinases.
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pubmed:affiliation |
Howard Hughes Medical Institute, Department of Medicine (Cardiology), Duke University Medical Center, Durham, North Carolina 27710, USA. pitch001@mc.duke.edu
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Review
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