Oxyntomodulin differentially affects glucagon-like peptide-1 receptor beta-arrestin recruitment and signaling through Galpha(s)

Research output: Contribution to journal › Journal article › Research › peer-review

Standard

Oxyntomodulin differentially affects glucagon-like peptide-1 receptor beta-arrestin recruitment and signaling through Galpha(s). / Jorgensen, Rasmus; Kubale, Valentina; Vrecl, Milka; Schwartz, Thue W; Elling, Christian E.

In: Journal of Pharmacology and Experimental Therapeutics, Vol. 322, No. 1, 2007, p. 148-54.

Research output: Contribution to journal › Journal article › Research › peer-review

Harvard

Jorgensen, R, Kubale, V, Vrecl, M, Schwartz, TW & Elling, CE 2007, 'Oxyntomodulin differentially affects glucagon-like peptide-1 receptor beta-arrestin recruitment and signaling through Galpha(s)', Journal of Pharmacology and Experimental Therapeutics, vol. 322, no. 1, pp. 148-54. https://doi.org/10.1124/jpet.107.120006

APA

Jorgensen, R., Kubale, V., Vrecl, M., Schwartz, T. W., & Elling, C. E. (2007). Oxyntomodulin differentially affects glucagon-like peptide-1 receptor beta-arrestin recruitment and signaling through Galpha(s). Journal of Pharmacology and Experimental Therapeutics, 322(1), 148-54. https://doi.org/10.1124/jpet.107.120006

Vancouver

Jorgensen R, Kubale V, Vrecl M, Schwartz TW, Elling CE. Oxyntomodulin differentially affects glucagon-like peptide-1 receptor beta-arrestin recruitment and signaling through Galpha(s). Journal of Pharmacology and Experimental Therapeutics. 2007;322(1):148-54. https://doi.org/10.1124/jpet.107.120006

Author

Jorgensen, Rasmus ; Kubale, Valentina ; Vrecl, Milka ; Schwartz, Thue W ; Elling, Christian E. / Oxyntomodulin differentially affects glucagon-like peptide-1 receptor beta-arrestin recruitment and signaling through Galpha(s). In: Journal of Pharmacology and Experimental Therapeutics. 2007 ; Vol. 322, No. 1. pp. 148-54.

Bibtex

@article{844012b0b44c11df825b000ea68e967b,
title = "Oxyntomodulin differentially affects glucagon-like peptide-1 receptor beta-arrestin recruitment and signaling through Galpha(s)",
abstract = "The glucagon-like peptide (GLP)-1 receptor is a promising target for the treatment of type 2 diabetes and obesity, and there is great interest in characterizing the pharmacology of the GLP-1 receptor and its ligands. In the present report, we have applied bioluminescence resonance energy transfer assays to measure agonist-induced recruitment of betaarrestins and G-protein-coupled receptor kinase (GRK) 2 to the GLP-1 receptor in addition to traditional measurements of second messenger generation. The peptide hormone oxyntomodulin is described in the literature as a full agonist on the glucagon and GLP-1 receptors. Surprisingly, despite being full agonists in GLP-1 receptor-mediated cAMP accumulation, oxyntomodulin and glucagon were observed to be partial agonists in recruiting betaarrestins and GRK2 to the GLP-1 receptor. We suggest that oxyntomodulin and glucagon are biased ligands on the GLP-1 receptor.",
author = "Rasmus Jorgensen and Valentina Kubale and Milka Vrecl and Schwartz, {Thue W} and Elling, {Christian E}",
note = "Keywords: Animals; Arrestins; COS Cells; Cercopithecus aethiops; Cyclic AMP; G-Protein-Coupled Receptor Kinase 2; G-Protein-Coupled Receptor Kinase 5; GTP-Binding Protein alpha Subunits, Gs; Glucagon; Glucagon-Like Peptide 1; Humans; Luminescent Measurements; Oxyntomodulin; Protein-Serine-Threonine Kinases; Receptors, Glucagon; Signal Transduction; beta-Adrenergic Receptor Kinases",
year = "2007",
doi = "10.1124/jpet.107.120006",
language = "English",
volume = "322",
pages = "148--54",
journal = "Journal of Pharmacology and Experimental Therapeutics",
issn = "0022-3565",
publisher = "American Society for Pharmacology and Experimental Therapeutics",
number = "1",

}

RIS

TY - JOUR

T1 - Oxyntomodulin differentially affects glucagon-like peptide-1 receptor beta-arrestin recruitment and signaling through Galpha(s)

AU - Jorgensen, Rasmus

AU - Kubale, Valentina

AU - Vrecl, Milka

AU - Schwartz, Thue W

AU - Elling, Christian E

N1 - Keywords: Animals; Arrestins; COS Cells; Cercopithecus aethiops; Cyclic AMP; G-Protein-Coupled Receptor Kinase 2; G-Protein-Coupled Receptor Kinase 5; GTP-Binding Protein alpha Subunits, Gs; Glucagon; Glucagon-Like Peptide 1; Humans; Luminescent Measurements; Oxyntomodulin; Protein-Serine-Threonine Kinases; Receptors, Glucagon; Signal Transduction; beta-Adrenergic Receptor Kinases

PY - 2007

Y1 - 2007

N2 - The glucagon-like peptide (GLP)-1 receptor is a promising target for the treatment of type 2 diabetes and obesity, and there is great interest in characterizing the pharmacology of the GLP-1 receptor and its ligands. In the present report, we have applied bioluminescence resonance energy transfer assays to measure agonist-induced recruitment of betaarrestins and G-protein-coupled receptor kinase (GRK) 2 to the GLP-1 receptor in addition to traditional measurements of second messenger generation. The peptide hormone oxyntomodulin is described in the literature as a full agonist on the glucagon and GLP-1 receptors. Surprisingly, despite being full agonists in GLP-1 receptor-mediated cAMP accumulation, oxyntomodulin and glucagon were observed to be partial agonists in recruiting betaarrestins and GRK2 to the GLP-1 receptor. We suggest that oxyntomodulin and glucagon are biased ligands on the GLP-1 receptor.

AB - The glucagon-like peptide (GLP)-1 receptor is a promising target for the treatment of type 2 diabetes and obesity, and there is great interest in characterizing the pharmacology of the GLP-1 receptor and its ligands. In the present report, we have applied bioluminescence resonance energy transfer assays to measure agonist-induced recruitment of betaarrestins and G-protein-coupled receptor kinase (GRK) 2 to the GLP-1 receptor in addition to traditional measurements of second messenger generation. The peptide hormone oxyntomodulin is described in the literature as a full agonist on the glucagon and GLP-1 receptors. Surprisingly, despite being full agonists in GLP-1 receptor-mediated cAMP accumulation, oxyntomodulin and glucagon were observed to be partial agonists in recruiting betaarrestins and GRK2 to the GLP-1 receptor. We suggest that oxyntomodulin and glucagon are biased ligands on the GLP-1 receptor.

U2 - 10.1124/jpet.107.120006

DO - 10.1124/jpet.107.120006

M3 - Journal article

C2 - 17395766

VL - 322

SP - 148

EP - 154

JO - Journal of Pharmacology and Experimental Therapeutics

JF - Journal of Pharmacology and Experimental Therapeutics

SN - 0022-3565

IS - 1

ER -

ID: 21666285