Mutation4-a | Helix/Position4-b | Effect on Ligand Binding and Signal Transduction | Reference |
---|---|---|---|
V11I | 1.36 | No changes in (radio)ligand binding | Beukers et al., 2000 |
A12T | 1.37 | No changes in (radio)ligand binding | Beukers et al., 2000 |
L58V | 2.55 | No changes in (radio)ligand binding | Beukers et al., 2000 |
F59L | 2.56 | No specific radioligand binding and no cAMP production | Beukers et al., 2000 |
N273Y | 7.36 | Up 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).