Development and Characterization of a Fluorescent Tracer for the Free Fatty Acid Receptor 2 (FFA2/GPR43)

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

Standard

Development and Characterization of a Fluorescent Tracer for the Free Fatty Acid Receptor 2 (FFA2/GPR43). / Hansen, Anders Højgaard; Sergeev, Eugenia; Pandey, Sunil K.; Hudson, Brian D; Rexen Ulven, Elisabeth; Milligan, Graeme; Ulven, Trond.

In: Journal of Medicinal Chemistry, Vol. 60, No. 13, 2017, p. 5638-5645.

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

Harvard

Hansen, AH, Sergeev, E, Pandey, SK, Hudson, BD, Rexen Ulven, E, Milligan, G & Ulven, T 2017, 'Development and Characterization of a Fluorescent Tracer for the Free Fatty Acid Receptor 2 (FFA2/GPR43)', Journal of Medicinal Chemistry, vol. 60, no. 13, pp. 5638-5645. https://doi.org/10.1021/acs.jmedchem.7b00338

APA

Hansen, A. H., Sergeev, E., Pandey, S. K., Hudson, B. D., Rexen Ulven, E., Milligan, G., & Ulven, T. (2017). Development and Characterization of a Fluorescent Tracer for the Free Fatty Acid Receptor 2 (FFA2/GPR43). Journal of Medicinal Chemistry, 60(13), 5638-5645. https://doi.org/10.1021/acs.jmedchem.7b00338

Vancouver

Hansen AH, Sergeev E, Pandey SK, Hudson BD, Rexen Ulven E, Milligan G et al. Development and Characterization of a Fluorescent Tracer for the Free Fatty Acid Receptor 2 (FFA2/GPR43). Journal of Medicinal Chemistry. 2017;60(13):5638-5645. https://doi.org/10.1021/acs.jmedchem.7b00338

Author

Hansen, Anders Højgaard ; Sergeev, Eugenia ; Pandey, Sunil K. ; Hudson, Brian D ; Rexen Ulven, Elisabeth ; Milligan, Graeme ; Ulven, Trond. / Development and Characterization of a Fluorescent Tracer for the Free Fatty Acid Receptor 2 (FFA2/GPR43). In: Journal of Medicinal Chemistry. 2017 ; Vol. 60, No. 13. pp. 5638-5645.

Bibtex

@article{bf3514f373134196a8ec3eb281ac830b,
title = "Development and Characterization of a Fluorescent Tracer for the Free Fatty Acid Receptor 2 (FFA2/GPR43)",
abstract = "The free fatty acid receptor 2 (FFA2/GPR43) is considered a potential target for treatment of metabolic and inflammatory diseases. Here we describe the development of the first fluorescent tracer for FFA2 intended as a tool for assessment of thermodynamic and kinetic binding parameters of unlabeled ligands. Starting with a known azetidine FFA2 antagonist, we used a carboxylic acid moiety known not to be critical for receptor interaction as attachment point for a nitrobenzoxadiazole (NBD) fluorophore. This led to the development of 4 (TUG-1609), a fluorescent tracer for FFA2 with favorable spectroscopic properties and high affinity, as determined by bioluminescence resonance energy transfer (BRET)-based saturation and kinetic binding experiments, as well as a high specific to nonspecific BRET binding signal. A BRET-based competition binding assay with 4 was also established and used to determine binding constants and kinetics of unlabeled ligands.",
author = "Hansen, {Anders H{\o}jgaard} and Eugenia Sergeev and Pandey, {Sunil K.} and Hudson, {Brian D} and {Rexen Ulven}, Elisabeth and Graeme Milligan and Trond Ulven",
year = "2017",
doi = "10.1021/acs.jmedchem.7b00338",
language = "English",
volume = "60",
pages = "5638--5645",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "13",

}

RIS

TY - JOUR

T1 - Development and Characterization of a Fluorescent Tracer for the Free Fatty Acid Receptor 2 (FFA2/GPR43)

AU - Hansen, Anders Højgaard

AU - Sergeev, Eugenia

AU - Pandey, Sunil K.

AU - Hudson, Brian D

AU - Rexen Ulven, Elisabeth

AU - Milligan, Graeme

AU - Ulven, Trond

PY - 2017

Y1 - 2017

N2 - The free fatty acid receptor 2 (FFA2/GPR43) is considered a potential target for treatment of metabolic and inflammatory diseases. Here we describe the development of the first fluorescent tracer for FFA2 intended as a tool for assessment of thermodynamic and kinetic binding parameters of unlabeled ligands. Starting with a known azetidine FFA2 antagonist, we used a carboxylic acid moiety known not to be critical for receptor interaction as attachment point for a nitrobenzoxadiazole (NBD) fluorophore. This led to the development of 4 (TUG-1609), a fluorescent tracer for FFA2 with favorable spectroscopic properties and high affinity, as determined by bioluminescence resonance energy transfer (BRET)-based saturation and kinetic binding experiments, as well as a high specific to nonspecific BRET binding signal. A BRET-based competition binding assay with 4 was also established and used to determine binding constants and kinetics of unlabeled ligands.

AB - The free fatty acid receptor 2 (FFA2/GPR43) is considered a potential target for treatment of metabolic and inflammatory diseases. Here we describe the development of the first fluorescent tracer for FFA2 intended as a tool for assessment of thermodynamic and kinetic binding parameters of unlabeled ligands. Starting with a known azetidine FFA2 antagonist, we used a carboxylic acid moiety known not to be critical for receptor interaction as attachment point for a nitrobenzoxadiazole (NBD) fluorophore. This led to the development of 4 (TUG-1609), a fluorescent tracer for FFA2 with favorable spectroscopic properties and high affinity, as determined by bioluminescence resonance energy transfer (BRET)-based saturation and kinetic binding experiments, as well as a high specific to nonspecific BRET binding signal. A BRET-based competition binding assay with 4 was also established and used to determine binding constants and kinetics of unlabeled ligands.

U2 - 10.1021/acs.jmedchem.7b00338

DO - 10.1021/acs.jmedchem.7b00338

M3 - Journal article

C2 - 28570808

VL - 60

SP - 5638

EP - 5645

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

SN - 0022-2623

IS - 13

ER -

ID: 189161714