Betablockers at Work: The Crystal Structure of the β2‐Adrenergic Receptor

Abstract

Rational drug design is still limited for many membrane proteins. For the β2-adrenergic receptor, a prototype of the class A GPCR family, structures with up to 2.4-Å resolution have now been solved. The structure (see figure) shows detailed contacts of the receptor (green) with its ligand carazolol (pink), and makes possible the formulation of hypotheses for the mode of action of G-protein-coupled receptors.