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Recent Progress in Understanding of Structure, Ligand Interactions and the Mechanism of Activation of the β 2-Adrenergic Receptor

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Abstract:

The understanding of β2-adrenergic receptor (β2AR) 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 β2AR 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 β-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.





Keywords: GPCRs; allosteric manner; biased agonism; crystal structure; molecular switches; peptides, or proteins; receptor activation; signaling pathways; β-adrenoceptors; β2AR

Document Type: Research Article

DOI: http://dx.doi.org/10.2174/092986712799320547

Publication date: March 1, 2012

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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