Table 1.
Averaged rmsds (Å) of the 7TM bundle pairs in the inactive state for class A GPCRs of known structure.
Figure 1.
Stereo view of molecular overlay of 10 representative 7TM bundles of inactivated GPCRs of known structure.
a) The extracellular side is facing upward while helix I is shown on the left. b) The 7TM bundles are viewed from the bottom of a). Seven highly conserved residues (*.50 s) are shown on the Cα backbone traces. The colors of receptors are red, bovine rhodopsin (1U19-A); pink, squid rhodopsin (2Z73-A); blue, β2 receptor (2RH1); cyan, β1 receptor (2VT4-B); yellow, A2A receptor (3EML); gray, CXCR4 receptor (3ODU-A); magenta, D3 receptor (3PBL-A); purple, H1 receptor (3RZE); green, M2 receptor (3UON); light green, S1P1 receptor (3V2Y).
Figure 2.
Averaged displacement (Å) of Cα atoms of 200 residues.
Thirty-six pairwise deviations at each position were averaged and plotted against a serial number of residues in a 7TM bundle. The residues located in the same section (slab) are colored in red, section 1; pink, section 2; green, section 3; cyan, section 4; blue, section 5. The borders between the adjacent helices are shown with gray bars at the top of the panel, while the positions of seven *.50 residues are shown with short black bars near the zero line of the graph.
Figure 3.
Molecular overlay of section 1 of 10 representative chains of inactivated GPCRs of known structure.
All the polypeptides (thin lines) and bound ligands (thick lines) are viewed (a) perpendicularly (from the cytoplasmic side) or (b) horizontally (from the top of a), parallel to the membrane). Backbone ribbons of β2 receptor are also shown to clarify the position of the 7 helices. Colors of the side chains and ligands of each receptor are the same as in Figure 1. The Cα backbone trace of bovine rhodopsin is marked with a red asterisk in a).
Figure 4.
Projection view (from the cytoplasmic side) of molecular overlay of sections 1 and 2.
a) 10 representative chains of inactivated GPCRs. b) the same inactive chains plus 2 chains of activated bovine rhodopsin. The colors in a) are the same as in Figure 1. In b), 1 inactivated chain (1U19-A) and 2 activated chains of bovine rhodopsin (PDB ID: 3PQR and 3PXO) are shown in red and black, respectively, while other chains are shown in gray.