Figure 8. A2BR’s C-terminal PDZ motif confers selective enhancement of GPCR function in the presence of CFTR.
(A) The last 4 amino acids on A2BR and β2AR are predicted PDZ-binding motifs. The cartoon depicts both wild-type A2BR and β2AR; A2BR where the last 4 amino acids were replaced with those from β2AR (A2BRDSLL); and β2AR with the last 4 amino acids from A2BR (β2ARGVGL). Mean changes in FRET between CFTRcfp and (B) wild-type A2BRGVGLyfp or A2BRDSLLyfp and (C) wild-type β2ARDSLLyfp and β2ARGVGLyfp measured in BHK cells. n = 7, 11, 12 and 14 for each pair respectively. Open bars, vehicle; closed bars, ADO; gray bars, ISO. Relative increase in intracellular cAMP levels (agonist/vehicle) for (D) A2BR and (E) β2AR transfected into BHKCFTR cells as indicated. N = 5, 11, 6 and 12 respectively. *p < 0.05 different from vehicle. †p < 0.05 different to wild-type or different ± CFTR.