Sci. Signal., 6 March 2012
Structural Biology Choosing a Path
Science, AAAS, Washington, DC 20005, USA
The β2-adrenergic receptor (β2AR) is a G protein–coupled receptor that recognizes diverse ligands to trigger signaling in the cell. Besides binding G proteins, activated β2AR can be phosphorylated and bind arrestin, which redirects signaling to other pathways. Some β2AR ligands are "biased" in that they differentially activate G protein or arrestin signaling. Liu et al. (see the Perspective by Sprang and Chief Elk) used fluorine-19 nuclear magnetic resonance (19F-NMR) spectroscopy to examine conformational changes associated with a range of ligands and discovered that biased ligands caused differential shifts in equilibrium between two conformational states—the G protein binding state and the arrestin binding state—and thus provide a basis for rational design of pharmacological ligands.
Citation: V. Vinson, Choosing a Path. Sci. Signal. 5, ec74 (2012).
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