Specific activation of Gs by synthetic peptides corresponding to an intracellular loop of the β‐adrenergic receptor

FEBS Letters

Strader, Catherine D.¹  Graziano, Michael P.¹  Huang, Ruey-Ruey C.¹  Cheung, Anne H.¹ 

[1]Department of Molecular Pharmacology and Biochemistry, Merck, Sharp and Dohme Research Laboratories, Rahway, NJ 07065, USA

关键词: Receptor;    G-protein;    Peptide;    GTP;    Amphiphilic sequence;   

DOI  :  10.1016/0014-5793(91)80167-2

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Peptides corresponding to the amino acid sequence of the hamster β₂-adrenergic receptor (β₂AR) were synthesized and their ability to activate purified G-proteins determined. Two peptides, comprising the N- and C-terminal 15 amino acids of the putative third intracellular loop region of the β₂AR were found to activate the G-protein G_s but not to activate a preparation of G_i/G_o. Other peptides corresponding to the internal portions of this loop and the C-terminal tail region failed to activate either G-protein. The presence of phospholipid vesicles was required for this activation. The observation that peptides with sequences corresponding to the ends of the third intracellular loop of the βAR can specifically activate G_s confirms the results of previous mutagenesis studies on the receptor and demonstrates that the secondary structure conferred by the amino acid sequences in these regions is sufficient for the activation of G-proteins.

【 授权许可】

Unknown