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. 2024 Jan 29;14(5):2137–2152. doi: 10.1016/j.apsb.2024.01.014

Figure 1.

Figure 1

In vitro validation of the conjugates' selectivity and activity. (A) Dual luciferase ER reporter system in the HEK-293 cells. (B) ERα luciferase reporter activity. n = 5 (Vehicle, E2, VB-l65, JW-127); n = 4 (JW-191). All the compounds were at 1 mmol/L. (C–E) ERβ luciferase activity. (C) Comparing the ERβ activity of the conjugates. n = 5 (Vehicle, E2, VB-l65, JW-127), n = 4 (JW-191). (D) Assessing activity of the conjugates in the presence of both ERα and ERβ. n = 4 for all groups. The symbol “#” was denoted for statistical comparisons between the same treatment groups under the presence of either ERβ overexpression or both ERα and ERβ, ##P < 0.01, ###P < 0.001. (E) JW-127 dose response. n = 3 (Vehicle, E2: 1 mmol/L, JW-127: 0.3 mmol/L, JW-127: 1 mmol/L), n = 5 (JW-127: 3 mmol/L). (F) JW-191 dose response. n = 3 for all groups. E2, estradiol. PPT, subtype selective ERα agonist. ∗P < 0.05, ∗∗P < 0.01, ∗∗∗P < 0.001, ∗∗∗∗P < 0.0001, n.s., not significant. All values are presented as the mean ± SEM.