Fig. 5: Homeostatic scaling of MOR responses by GPR139.
From: Homeostatic scaling of dynorphin signaling by a non-canonical opioid receptor
a Schematic of cAMP signaling platform to study the influence of GPR139 co-expression on MOR activation by different ligands. b Concentration-response curve for DAMGO-mediated MOR activation with or without GPR139 co-expression. c Concentration-response curve for DAMGO-mediated MOR activation with or without GPR139 co-expression in the presence of 10 μM JNJ-63533054. d Maximum efficacy of DAMGO-mediated activation of MOR and MOR co-expressed with GPR139. e The negative logarithm of the EC50 (pEC50) of DAMGO-mediated activation of MOR with and without GPR139 co-expression. f Concentration-response curve for Dyn A13-mediated MOR activation with or without GPR139 co-expression. g Maximum efficacy of Dyn A13-mediated activation of MOR and MOR upon co-expression with GPR139. h The negative logarithm of the EC50 (pEC50) of Dyn A13-mediated activation of MOR and MOR upon co-expression with GPR139. i Schematic of luminescence complementation assay to detect change in cell surface abundance of MOR. Time course of changes in MOR cell surface abundance upon treatment with DAMGO (j) and Dyn A13 (k). Quantification of MOR internalization by DAMGO (l) and Dyn A13 (n). Quantification of MOR internalization rate in response to DAMGO (m) and Dyn A13 (o). Data shown are mean ± SEM of n = 3 independent experiments. Data were analyzed by d two-way ANOVA with Fisher’s least significant difference test, e one-way ANOVA with Dunnett’s test or (g, h, l, m, n, o) unpaired two-tailed t-test. *p < 0.05, **p < 0.01 and ***p < 0.001, n.s. p > 0.05.
