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Comment
. 2012 Mar 2;335(6072):1055-6.
doi: 10.1126/science.1219302.

Cell signaling. Structural origins of receptor bias

Stephen R Sprang  1 , Jackson Chief Elk
Affiliations
Comment

Cell signaling. Structural origins of receptor bias

Stephen R Sprang et al. Science. .

Abstract

Agonists can elicit pathway-specific conformational changes in a G protein–coupled receptor.

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Figures

Figure 1
Figure 1. Functionally selective
Binding of agonists to the β2AR results in conformational changes that displace TM5 and TM6 (green) and/or TM7 (blue). The conformational changes permit G protein (Gs) binding or receptor phosphorylation (P) and β-arrestin binding. β-arrestin binding blocks G protein signaling. The aromatic moiety of the agonist (isoproterenol shown) contacts TM5 and TM6, whereas the hydroxylamine substituent interacts with TM3 and TM7.
See this image and copyright information in PMC

Comment on

References

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