Fig. 4: DP1 activation mechanism.

a, b Comparison of the inactive (blue) and active (salmon) states of DP1, viewed within the plane of the membrane (a) and from the intracellular side (b). Red arrows indicate main conformational shifts of TMs on the intracellular side of the receptor. The membrane boundaries are shown in (a) as two gray lines. c–f Structural details of activation-related motifs in DP1, showing the ligand binding pocket (c), the T5.52-L3.43-F6.44 motif (d), the sodium-binding site (e), the EC3.50W and DP7.50xxF motifs (f). The ligands in (a–f) are shown as sticks with carbon atoms colored in gold (PGD2) or cyan (ONO3030297). g MD analysis of K762.54 interactions with D722.50 and PGD2. h ONE-GO Gs signaling assay comparing the concentration-response signal induced by PGD2 at WT DP1 with activation-related mutants. The data are normalized to the basal signal (set at 0%) and the maximal PGD2-induced signal at WT DP1 (set at 100%). Data points correspond to means ± SEM for three biologically independent experiments conducted in triplicates. The corresponding Emax and EC50 values are shown in Supplementary Table 2. Source Data are provided as a Source data file.