Antisense oligonucleotides against receptor kinase GRK2 disrupt target selectivity of β‐adrenergic receptors in atrial myocytes

FEBS Letters

Bender, Kirsten¹  Brandts, Bodo¹  Pott, Lutz¹  Wellner-Kienitz, Marie-Cécile¹  Meyer, Thomas¹ 

[1] Institut für Physiologie, Abteilung Zelluläre Physiologie, Ruhr-Universität Bochum, D-44780 Bochum, Germany

关键词: Potassium channel;    GIRK;    G-protein;    β-receptor;    GRK2;    Antisense;   

DOI  :  10.1016/S0014-5793(99)00594-3

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

K⁺ channels composed of GIRK subunits are predominantly expressed in the heart and various regions of the brain. They are activated by βγ-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 G_βγ binding sites, in a fraction of cells, K_(ACh) channels can be activated by β-adrenergic receptors. Sensitivity to β-agonist is insensitive to pertussis toxin treatment. These findings demonstrate a potential role of G_βγ binding proteins for target selectivity of G-protein-coupled receptors

【 授权许可】

Unknown