Fig. 3: Experimental data for OS5- and OS9-mutants in the M3R.
From: The pocketome of G-protein-coupled receptors reveals previously untargeted allosteric sites
The y-axis depicts the position of the pocket residues (Ballesteros-Weinstein numbering35). Grey lines linking the points connect the respective double and quadruple mutants. The left panel shows the difference between the mutant logEC50 and the mean wildtype (wt) logEC50 values (\({{{{{{{{\rm{logEC}}}}}}}}}_{50}^{{{{{{{{\rm{mut}}}}}}}}}-{{{{{{{{\rm{logEC}}}}}}}}}_{50}^{{{{{{{{\rm{wt}}}}}}}}}\)) and the right panel the normalised amplitude (Ampmut/Ampwt) of the extent to which β-arrestin2 was recruited. While in the left plot a value of 0 corresponds to no potency changes, a value of 1 in the right plot corresponds to no changes in efficacy compared to wt. The greyed out area indicates minimal and maximal potency shifts of multiple Gαq wt measurements. The central panel depicts interhelical residue contacts of each of the mutated residues that are important in active (blue) or inactive (red) conformations of class A GPCRs in a similar manner to Supplementary Fig. 10 (normalised PCA coefficient cut-off: 0.5). The point size correlates with the normalised PCA coefficient for a given contact and can be seen as a direct measurement of importance for a given state. Source data are provided as a source_data.xlsx file.
