Fig. 2: Characterization of MOR FRET-based receptor conformation sensor. | Communications Biology

Fig. 2: Characterization of MOR FRET-based receptor conformation sensor.

From: Dynamics of agonist-evoked opioid receptor activation revealed by FRET- and BRET-based opioid receptor conformation sensors

Fig. 2

A Averaged FRET-based measurement of HEK293 cells stably expressing MOR conformation sensor measured in a 96-well plate format (schematic image of a 96-well plate created with BioRender, licence INC-12457) at a plate reader. Increasing concentrations of DAMGO were applied followed by a saturating concentration of DAMGO and the antagonist naloxone. The agonist-induced activation was normalized to the maximal activation and plotted as concentration–response curve (B) (mean ± SEM, n = 3 of independent transfections measured in triplets). B, C Concentration–response (B) and inhibition (C) curves for the FRET MOR sensor (IC50: 2.7 nM; pKi: 1.1 nM). D, E Averaged BRET-based measurement (D) of HEK293T cells expressing MOR-nLuc, mCit-Arrestin3 and GRK2. Increasing concentrations of DAMGO were applied followed by a saturating concentration of DAMGO. The agonist-induced activation was normalized to the max. activation and plotted as concentration–response curve (E) (mean ± SEM, n = 3 of independent transfections measured in triplets). F, G Averaged BRET-based measurement (F) of HEK293T cells expressing MOR and Go-case BRET-sensor. Increasing concentrations of DAMGO were applied followed by a saturating concentration of DAMGO. The agonist-induced activation was normalized to the max. activation and plotted as concentration–response curve (G) (mean ± SEM, n = 3 of independent transfections measured in triplets).

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