Figure 1 | Scientific Reports

Figure 1

From: Ternary crystal structure of human RORγ ligand-binding-domain, an inhibitor and corepressor peptide provides a new insight into corepressor interaction

Figure 1

The relative efficacy (RE) of CoR peptide recruitment to the RORγ-LBD and LUC activity by inverse agonists. (A) Chemical structures of compound A and T. (B) Inverse agonist activities in FRET assays and LUC reporter assay. Inlet figure shows the CoA-releasing activities of inverse agonists. REs of CoR recruitment and CoA releasing are shown as percent activation relative to that of standard compound 19. Background activity in the absence of a standard inverse agonist is defined as 0% response; and maximum activity induced by a standard inverse agonist at 100μM as 100% response. Dose-response curves are representative of independent results for each compound in LUC assay (Supplementary Fig. S1). A value of 100% is given to cells without inverse agonist in LUC assay. Data represent the means ± SE (n = 2–3), but not for data of compound T in FRET assay (n = 1).

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