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. 2013 Dec 5;110(52):E5088–E5097. doi: 10.1073/pnas.1312515110

Fig. 5.

Fig. 5.

ATI-2341 promotes a weak recruitment of β-arrestin to CXCR4. (A) BRET titration curves were performed in cells cotransfected with a constant amount of CXCR4-RlucII and increasing amounts of GFP2–β-arrestin2. Cells were stimulated with 500 nM SDF-1, 1 μM pepducins (ATI-2341, ATI-2339, or ATI-2504), or vehicle (Hanks) for 10 min before BRET was measured following coel-400a addition using the BRET480-YFP filter set. The curves shown are derived from individual titration curves that are representative of three independent experiments. The error bars represent the mean ± SD from duplicate wells. (B) Kinetics of the ligand-promoted BRET between CXCR4-RlucII and GFP2–β-arrestin2. BRET was measured at the indicated times following the addition of 500 nM SDF-1 or 1 μM pepducins. Data shown are the mean ± SEM of four independent experiments. (C) Effect of increasing concentrations of SDF-1 or ATI-2341 on the BRET between CXCR4-RlucII and GFP2–β-arrestin2. BRET was measured 10 min following the addition of ligands (EC50: ATI-2341, 273.5 ± 78.6 nM vs. SDF-1, 1.8 ± 0.3 nM). (Inset) The y axis scale enlargement for better visibility. Data shown are the mean ± SEM of seven independent experiments.