Figure 7.
Conversion of arginine172 to alanine or lysine eliminates agonism of orthosteric agonists but not of DIM. (a) Membranes expressing either GPR84-Cys352IleGαi2, Arg172Ala GPR84-Cys352IleGαi2 or Arg172Lys GPR84-Cys352IleGαi2 were used in [35S]GTPγS binding studies to assess function of (ai) DIM, (aii), C10, (aiii) embelin and (aiv) compound-1. (b) Similar studies were performed on membrane of cells induced to express FLAG-hGPR84-eYFP (bi), FLAG-Arg172Ala hGPR84-eYFP (bii), FLAG-Arg174Ala hGPR84-eYFP (biii) to assess activity of C10, DIM, embelin and compound-1.