Linked Life Data

16339846

Source:http://linkedlifedata.com/resource/pubmed/id/16339846

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
3
pubmed:dateCreated
2006-2-16
pubmed:abstractText
The defining characteristic of G protein-coupled receptor homologous desensitization is that the receptor must be occupied by an agonist or in an activated conformation that mimics an agonist-induced state. In most instances, the mechanistic basis for this characteristic is the high selectivity of G protein-coupled receptor kinases for the activated receptor. In this issue, Rankin et al. (p. 759) demonstrate that under some conditions, at least, the G protein-coupled receptor kinase GRK4 does not display a preference for the agonist-occupied D1 dopamine receptor. Coexpression of GRK4 and the D1 receptor in a heterologous system induces phosphorylation of the receptor in the absence of agonist, causing constitutive desensitization and internalization of the receptor. Lacking the normal rapid feedback mechanisms associated with homologous desensitization, a system incorporating constitutively active GRK4 will be prone to dysregulation, perhaps explaining the generally low expression of GRK4. Indeed, considerable evidence suggests that just such dysregulation resulting from mutationally activated GRK4 contributes to the heritable component of human essential hypertension (Physiol Genomics 19:223-246, 2004).
pubmed:commentsCorrections
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Mar
pubmed:issn
0026-895X
pubmed:author
pubmed:issnType
Print
pubmed:volume
69
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
673-6
pubmed:dateRevised
2007-11-15
pubmed:meshHeading
pubmed:year
2006
pubmed:articleTitle
Novel features of G protein-coupled receptor kinase 4.
pubmed:affiliation
Department of Behavioral Neuroscience, Oregon Health & Science University, Portland, USA. nevek@ohsu.edu
pubmed:publicationType
Journal Article, Comment