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A Dynamic, Split-Luciferase-Based Mini-G Protein Sensor to Functionally Characterize Ligands at All Four Histamine Receptor Subtypes

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Höring, Carina ; Seibel, Ulla ; Tropmann, Katharina ; Grätz, Lukas ; Mönnich, Denise ; Pitzl, Sebastian ; Bernhardt, Günther ; Pockes, Steffen ; Strasser, Andrea
License: Creative Commons Attribution 4.0
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Date of publication of this fulltext: 13 Jan 2021 15:04


In drug discovery, assays with proximal readout are of great importance to study target-specific effects of potential drug candidates. In the field of G protein-coupled receptors (GPCRs), the determination of GPCR-G protein interactions and G protein activation by means of radiolabeled GTP analogs ([S-35]GTP gamma S, [gamma-P-32]GTP) has widely been used for this purpose. Since we were repeatedly ...


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