Fig. 1: Activation of PAR1 and cryo-EM structures of TA–PAR1–Gq and TA–PAR1–Gi complexes.
From: Structural basis of tethered agonism and G protein coupling of protease-activated receptors
a PAR1 is cleaved by thrombin at the N-terminus which exposes the TA, SFLLRN, which can bind and activate PAR1, arousing several G protein signaling pathways, including Gq, G12/13 and Gi leading to platelet activation and aggregation. b, c Cryo-EM map (b) and model (c) of the TA–PAR1–Gq complex. The TA is shown in orange, PAR1 in teal, Gαq in yellow, Gβ in purple, Gγ in dark magenta, and scFv16 in gray. d, e Cryo-EM map (d) and model (e) of the TA–PAR1–Gi complex. The TA is shown in light green, PAR1 in pink, Gαi in blue, Gβ in purple, Gγ in dark magenta, and scFv16 in gray.
