RGD Reference Report - Phosphorylation and desensitization of alpha1d-adrenergic receptors. - Rat Genome Database

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Phosphorylation and desensitization of alpha1d-adrenergic receptors.

Authors: Garcia-Sainz, JA  Vazquez-Cuevas, FG  Romero-Avila, MT 
Citation: Garcia-Sainz JA, etal., Biochem J 2001 Feb 1;353(Pt 3):603-10.
RGD ID: 68202
Pubmed: PMID:11171057   (View Abstract at PubMed)
PMCID: PMC1221606   (View Article at PubMed Central)

In rat-1 fibroblasts stably expressing rat alpha(1d)-adrenoceptors, noradrenaline and PMA markedly decreased alpha(1d)-adrenoceptor function (noradrenaline-elicited increases in calcium in whole cells and [(35)S]guanosine 5'-[gamma-thio]triphosphate binding in membranes), suggesting homologous and heterologous desensitizations. Photoaffinity labelling, Western blotting and immunoprecipitation identified alpha(1d)-adrenoceptors as a broad band of 70-80 kDa. alpha(1d)-Adrenoceptors were phosphorylated in the basal state and noradrenaline and PMA increased it. The effect of noradrenaline was concentration-dependent (EC(50) 75 nM), rapid (maximum at 1 min) and transient. Phorbol ester-induced phosphorylation was concentration-dependent (EC(50) 25 nM), slightly slower (maximum at 5 min) and stable for at least 60 min. Inhibitors of protein kinase C decreased the effect of phorbol esters but not that of noradrenaline. Evidence of cross-talk of alpha(1d)-adrenoceptors with receptors endogenously expressed in rat-1 fibroblasts was given by the ability of endothelin, lysophosphatidic acid and bradykinin to induce alpha(1d)-adrenoceptor phosphorylation. In summary, it is shown for the first time here that alpha(1d)-adrenoceptors are phosphoproteins and that receptor phosphorylation is increased by the natural ligand, noradrenaline, by direct activation of protein kinase C and via cross-talk with other receptors endogenously expressed in rat-1 fibroblasts. Receptor phosphorylation has functional repercussions.

Gene Ontology Annotations    Click to see Annotation Detail View

Molecular Function
TermQualifierEvidenceWithReferenceNotesSourceOriginal Reference(s)
alpha1-adrenergic receptor activity  IDA 68202 RGD 

Objects Annotated

Genes (Rattus norvegicus)
Adra1d  (adrenoceptor alpha 1D)


Additional Information