Fig 1: Effect of AZD8797 on CX3CL1-induced [35S]GTPγS accumulation using CHO-hCX3CR1 membranesEach data point is the mean ± S.E.M. for at least 25 separate experiments. The y-axis is normalized to the percentage of [35S]GTPγS accumulation induced by 2 nM CX3CL1.
Fig 2: Effect of AZD8797 and CX3CL1 on 125I-CX3CL1 saturation binding to CHO-hCX3CR1 membranes(A) Specific binding of increasing concentrations of 125I-CX3CL1 in the presence of different concentrations of AZD8797. Each data point is the mean ± S.E.M. for two separate experiments. (B) Specific binding of increasing concentrations of 125I-CX3CL1 in the presence of different concentrations of CX3CL1. Data shown are representative averages and S.E.M. of duplicates from one of two separate experiments. (C) An affinity ratio plot of all 125I-CX3CL1 Kd values obtained in the presence of either CX3CL1 or AZD8797. Data for both CX3CL1 and AZD8797 were collected on two separate occasions. CX3CL1 linear fit slope 0.73 (0.52–0.93, 95% CL, n=2).
Fig 3: Effect of AZD8797 on β-arrestin recruitment induced by increasing concentrations of CX3CL1Data shown are representative averages and S.E.M. of duplicates from one of three separate experiments. The y-axis is normalized to the effect of 1 μM CX3CL1 as 100%.
Fig 4: Effect of CX3CL1 and AZD8797 on DMR with and without PTX treatmentEach data point is the mean ± S.E.M. for three separate experiments. (A) Effect of CX3CL1 on CHO-K1, CHO-hCX3CR1 and PTX-treated CHO-hCX3CR1 cells. (B) Effect of CX3CL1 on PTX-treated and untreated RPMI-8226 cells. (C) Effect of AZD8797 on CHO-K1, CHO-hCX3CR1 and PTX-treated CHO-hCX3CR1 cells. (D) Effect of AZD8797 on PTX-treated and untreated RPMI-8226 cells.
Fig 5: Saturation binding using CHO-hCX3CR1 membranes(A) 125I-CX3CL1 saturation binding using CHO-hCX3CR1 membranes alone and in the presence of 100 μM GTPγS. Each data point is the mean ± S.E.M. for four and two separate experiments respectively. (B) [3H]AZD8797 saturation binding using CHO-hCX3CR1 membranes. Each data point is the mean ± S.E.M. for four separate experiments.
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