Supplementary Figure 5 : Functional characterization of peptide ligands at the human μ-OR and δ-OR.

From: Structural basis for bifunctional peptide recognition at human δ-opioid receptor

Supplementary Figure 5

Efficacy and potency of the bi-functional ligand DIPP-NH2, the synthetic peptide ligand DAMGO as well as the endogenous opioid peptide endomorphin-1 and -2 were characterized at the μ-OR for arrestin recruitment using a BRET-based bioassay (a) and at the Gαi-protein pathway using a Glosensor-based bioassay (b). Results are reported as normalized concentration-responses induced by the selective μ-OR peptide ligand DAMGO. Similarly, the pharmacological profile of DIPP-NH2 toward the δ-OR was measured using a tango-based assay for arrestin recruitment (c,e) and Glosensor for Gαi activation (d,f). Normalized dose-response induced by the δ-OR peptide ligand DADLE is reported. e,f, Schild regression analysis at δ-OR arrestin recruitment and Gαi activity was performed with various concentration of DIPP-NH2 over a DADLE dose-response curve. Results represent mean ± SEM of three independent experiments each in quadruplicate.