Chapter 29

Fig. 29.2 Crystal structure of the human β2-adrenergic receptor with the bound agonist BI-167107 29.2. The receptor (red) could be crystallized with a bound Gs protein consisting of the α- (light blue), β- (purple) and γ-subunit (yellow). An antibody fragment was added to stabilize the structure, it is omitted from the figure. The binding pocket of the receptor containing the agonist BI-167107 29.2 is shown on the right. The ligand binds to Ser 203 on helix H3 via its lactam nitrogen and phenolic OH group. The OH group in the side chain interacts with Asn 312 on H7. The protonated nitrogen forms a salt bridge with Asp 113 on H3.