Fig. 1: Structure of S1P5 and its comparison with structures of other S1PRs: overview and conservative motifs.
From: Structural basis for receptor selectivity and inverse agonism in S1P5 receptors
a Superposition of the obtained in this work inactive S1P5 structure (pink cartoon) in complex with ONO-5430608 (purple spheres) with the inactive S1P1 (yellow cartoon)-ML056 (orange spheres) complex (PDB ID 3V2Y). b Superposition of the inactive S1P5-ONO-5430608 with the active S1P5 (violet cartoon)-siponimod (green spheres) complex (PDB ID 7EW1). Glycosylated residues and lipids observed in the S1P5-ONO-5430608 structure are shown as gray sticks. c Superposition of transmission switches for S1P5-ONO-5430608 (inactive state), S1P5-siponimod (active state), and S1P1-ML056 (inactive state). d Superposition of the DRY functional motif for the same three receptor-ligand pairs as in c. e Sequence conservation of the transmission switches and DRY motif in the S1PR family. Adenosine A2A receptor is included as a representative receptor of class A GPCR. f Sliced surface representation of known structures from the S1PR family with corresponding ligands: S1P1-ML056 (PDB ID 3V2Y), S1P3-S1P (PDB ID 7C4S), S1P5-siponimod (PDB ID 7EW1), and S1P5-ONO-5430608 (this work, PDB ID 7YXA).
