About the cover
August 2006 Volume 2 No 8
Coupling ligand structure to specific conformational switches in the 
2 adrenoceptor. Yao et al. (p 417)
showed that activation of the G protein-coupled receptor 2-AR is accompanied by at least two distinct molecular switches. The 'ionic lock' that holds together two of the transmembrane domains (red and blue) is broken upon receptor activation. Both the ionic lock switch
and a 'rotamer toggle switch', which modulates helix conformation around a conserved proline kink, are required for full receptor activation (see also News & Views by Vilardaga, p 395). The authors examined the effect of agonist structure on activation of these molecular switches. Cover art by Erin
Boyle based on imagery of 2-AR and small-molecule agonists provided by
Charles Parnot and Xavier Deupi.
2 adrenoceptor. Yao et al. (p 417)
showed that activation of the G protein-coupled receptor 2-AR is accompanied by at least two distinct molecular switches. The 'ionic lock' that holds together two of the transmembrane domains (red and blue) is broken upon receptor activation. Both the ionic lock switch
and a 'rotamer toggle switch', which modulates helix conformation around a conserved proline kink, are required for full receptor activation (see also News & Views by Vilardaga, p 395). The authors examined the effect of agonist structure on activation of these molecular switches. Cover art by Erin
Boyle based on imagery of 2-AR and small-molecule agonists provided by
Charles Parnot and Xavier Deupi. 