Antisense oligonucleotides against receptor kinase GRK2 disrupt target selectivity of beta-adrenergic receptors in atrial myocytes.
FEBS Lett
; 451(3): 279-83, 1999 May 28.
Article
in En
| MEDLINE
| ID: mdl-10371205
ABSTRACT
K+ channels composed of GIRK subunits are predominantly expressed in the heart and various regions of the brain. They are activated by betagamma-subunits released from pertussis toxin-sensitive G-proteins coupled to different seven-helix receptors. In rat atrial myocytes, activation of K(ACh) channels is strictly limited to receptors coupled to pertussis toxin-sensitive G-proteins. Upon treatment of myocytes with antisense oligodesoxynucleotides against GRK2, a receptor kinase with Gbetagamma binding sites, in a fraction of cells, K(ACh) channels can be activated by beta-adrenergic receptors. Sensitivity to beta-agonist is insensitive to pertussis toxin treatment. These findings demonstrate a potential role of Gbetagamma binding proteins for target selectivity of G-protein-coupled receptors.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Potassium Channels
/
Signal Transduction
/
Oligonucleotides, Antisense
/
Receptors, Adrenergic, beta
/
Cyclic AMP-Dependent Protein Kinases
/
Heart Atria
Limits:
Animals
Language:
En
Journal:
FEBS Lett
Year:
1999
Document type:
Article
Affiliation country:
Germany