Table 4

Mutational analysis of the human A2B AR with respect to ligand binding

Mutation4-aHelix/Position4-bEffect on Ligand Binding and Signal TransductionReference
V11I1.36No changes in (radio)ligand binding Beukers et al., 2000
A12T1.37No changes in (radio)ligand binding Beukers et al., 2000
L58V2.55No changes in (radio)ligand binding Beukers et al., 2000
F59L2.56No specific radioligand binding and no cAMP production Beukers et al., 2000
N273Y7.36Up to 60-fold increase in affinity of 2-substituted adenosines Beukers et al., 2000
• 4-a  Amino acids are represented in single-letter code with position number shown. The first amino acid is that of the wild-type receptor, and the second is the one used for substitution, based on the corresponding amino acid in the human A2A receptor.

• 4-b  Position on helix, using notation of van Rhee and Jacobson (1996).