Recent Progress in Understanding of Structure, Ligand Interactions and the Mechanism of Activation of the β2-Adrenergic Receptor.

TitleRecent Progress in Understanding of Structure, Ligand Interactions and the Mechanism of Activation of the β2-Adrenergic Receptor.
Publication TypeJournal Article
Year of Publication2012
AuthorsKoliński, Michał, Plazinska Anita, and Jozwiak Krzysztof
JournalCurrent medicinal chemistry
Date Published02/2012
ISSN1875-533X
AbstractThe understanding of b2-adrenergic receptor (b2AR) interactions with ligands as well as the mechanism of receptor activation changed radically from 2007, when the first crystallographic structure of the receptor was reported. Since then numerous crystallographic studies described interactions with all main classes of b2AR ligands and with G proteins, which provided a great insight into the molecular structure of the receptor. However, molecular mechanisms of receptor activations remain to be determined. Functional research supported the concept of ligand - directed signaling at b-adrenoceptors. Agonist can activate alternative signaling pathways with different capacities and trigger cellular effects. It indicates that agonists nominally belonging to the same class may bind to and/or stabilize different active conformations of the receptor which are selectively recognized by signaling proteins in the allosteric manner.