Two sites in the third inner loop of the dopamine D2 receptor are involved in functional G protein‐mediated coupling to adenylate cyclase

FEBS Letters

Palm, Dieter¹  Maiek, Daria¹  Münch, Gerald¹ 

[1] Theodor-Boveri-Institut für Biowissenschaften, Physiologische Chemie I, Universität Würzburg, W-8700 Würzburg, Germany

关键词: Dopamine D2 receptor;    G protein;    Receptor-G protein coupling;    Synthetic peptide;    G protein;    regulatory guanine nucleotide-binding protein;    Gs;    stimulatory G protein;    Gi;    o;    pertussis toxin sensitive G proteins;    gi;    transducin;    αAR;    βAR;    α-;    β-adrenergic receptor;    D2R;    dopamine D2 receptor;    MAChR;    muscarinic acetylcholin receptor;    PGE1;    prostaglandin E1;   

DOI  :  10.1016/0014-5793(93)81076-C

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Synthetic peptides, corresponding to the amino acid sequences of the N- and C-terminal parts of the 3rd intracellular loop of the dopamine D₂ receptor, attenuate dopaminergic adenylate cyclase inhibition in membranes. Both peptides also activate directly GTPase activity in membranes. We suggest a functional model for G_i-coupled receptors where two sites in the 3rd inner loop compose the links for the receptor-G protein interaction thus providing the tools for a selective and adjustable response. Functional coupling was not affected by a peptide representing the insert in the long form of the dopamine D; receptor (D_2(long)). The selectivity pattern of conventional G protein-linked receptors also sheds some light on the recently observed interaction of β-amyloid protein precursor (APP) complexes with G proteins.

【 授权许可】

Unknown