Fig. 4: Structural Comparison of Active and Inactive States of PAR2.
From: Structural basis for the activation of proteinase-activated receptors PAR1 and PAR2
A Overlay of the tethered ligand-bound active PAR2 (coral) and the antagonist AZ8838-bound inactive PAR2 (yellow; PDB 5NDD). The tethered peptide is colored in green spheres, while AZ8838 is shown in blue spheres. B Rotated extracellular view of the comparison between tethered ligand-bound active PAR2 (coral) and AZ8838-bound inactive PAR2 (yellow). C Conformations of key residues in inactive PAR2 (yellow) bound to the antagonist AZ8838 (blue) compared to active PAR2 (coral). D Detailed view of specific residues involved in H-bond rearrangements in the inactive (yellow) to active conformation (coral) of PAR2. E Detailed view of TM6 and TM7 highlighting residues that propagate agonist binding rearrangements in the active state (coral) compared to relative position in the inactive state (yellow). Red arrows denote steric forces applied by moving residues on neighboring residues.
