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Binding Sequence

Binding Diagram Left: Diagram showing amino acids involved in catecholamine binding to the beta 2 adrenergic receptor. Right: Three-dimensional model of the beta 2 adrenergic receptor as viewed from the cytoplasmic surface. The position of fluorescein bound to cysteine 265 (Cys265) is shown. Agonist binding leads to quenching of the fluorescence of fluorescein on Cys265.
Binding Sequence 1 Sequential binding model. The following three illustrations depict the binding of an agonist to the beta 2 adrenergic receptor. Only the transmembrane domains involved in agonist binding are shown. Our studies provide evidence for multiple agonist-specific conformational states and the existence of intermediate conformational states. In this panel the receptor is in the inactive state.
Binding Sequence 2 The agonist initially makes contact with two transmembrane domains and stabilizes an intermediate state.
Binding Sequence 3 Formation of the active state requires interactions between the agonist and all three transmembrane domains. This involves breaking a stabilizing interaction between the cytoplasmic ends of TM3 and TM6.

Movies

Binding Model Movie Movie depicting the sequential binding model.
Binding Model Movie Structure of the human beta 2 adrenergic receptor bound to carazolol. Obtained from the 2.4Å crystal structure of the beta2AR-T4lysozyme fusion protein.