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[Preprint]. 2024 Jul 16:rs.3.rs-4664764. [Version 1] doi: 10.21203/rs.3.rs-4664764/v1

Figure 3. CryoEM structures of δOR bound to bitopics.

Figure 3

A) Overall architecture of δOR-C6-Quino Gαi1Gβ1Gγ2 complex assembly. Density map of the ligand C6 is zoomed in. B) Comparison of C6-Quino bound δOR with previous inactive- and active-state δOR structure. δOR-naltrindole (PDB ID 4N6H), δOR-deltorphin (PDB ID 8F7S) C) Comparison of ligand binding pose between C6-Quino, naltrindole, and deltorphin. D) δOR-C6-Quino interactions in the orthosteric binding pocket. E) Residues with distinct effects on C6-Quino and DPDPE were characterized in BRET-G protein activation or arrestin recruitment assays. Potency and efficacy values are shown in Table S7.