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- W2336745856 abstract "The free fatty acid receptor 1 (FFA1/GPR40) is a potential target for treatment of type 2 diabetes. Although several potent agonists have been described, there remains a strong need for suitable tracers to interrogate ligand binding to this receptor. We address this by exploring fluorophore-tethering to known potent FFA1 agonists. This led to the development of 4, a high affinity FFA1 tracer with favorable and polarity-dependent fluorescent properties. A close to ideal overlap between the emission spectrum of the NanoLuciferase receptor tag and the excitation spectrum of 4 enabled the establishment of a homogeneous BRET-based binding assay suitable for both detailed kinetic studies and high throughput competition binding studies. Using 4 as a tracer demonstrated that the compound acts fully competitively with selected synthetic agonists but not with lauric acid and allowed for the characterization of binding affinities of a diverse selection of known FFA1 agonists, indicating that 4 will be a valuable tool for future studies at FFA1." @default.
- W2336745856 created "2016-06-24" @default.
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- W2336745856 date "2016-05-10" @default.
- W2336745856 modified "2023-09-24" @default.
- W2336745856 title "Development and Characterization of a Potent Free Fatty Acid Receptor 1 (FFA1) Fluorescent Tracer" @default.
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- W2336745856 doi "https://doi.org/10.1021/acs.jmedchem.6b00202" @default.
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