Adrenergic receptors are G protein-coupled receptors for epinephrine and norepinephrine. They are targets of many drugs for various conditions, including treatment of hypertension, hypotension, and asthma. Adrenergic receptors are intensively studied in structural biology, displayed for binding poses of different types of ligands. Here, we summarized molecular mechanisms of ligand recognition and receptor activation exhibited by structure. We also reviewed recent advances in structure-based ligand discovery against adrenergic receptors.
Keywords: GPCR; activation mechanism; adrenergic receptor; adrenoreceptor; allosteric modulator; aminergic receptor; receptor–ligand interactions; selectivity; structure-based drug design.