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. 2021 Aug 27;118(35):e2101657118. doi: 10.1073/pnas.2101657118

Fig. 5.

Fig. 5.

Activity of ligands in allele-specific models of tamoxifen resistance. (A–C) WT MCF7 cells and MCF7 cells engineered to express the mutant ERα-Y537S or ERα-D538G or overexpress EGFR were treated with the indicated SERM (16, 20) or SERD (27, 29) for 5 d and analyzed for inhibition of cell proliferation. Fulvestrant (Fulv). n = 3. Dashed lines indicate Emax values for 4OHT or fulvestrant (SI Appendix, Fig. S8). (D) MCF7-EGFR cells were treated with the indicated 1μM abemaciclib (Abe) and the indicated ligands for 5 d and analyzed for inhibition of cell proliferation. Fulvestrant (Fulv). n = 3. Dashed lines indicate Emax values for abemaciclib alone or fulvestrant (+Abe). (E and F) Structure-based model of tamoxifen and fulvestrant resistance. HepG2 liver cells were treated for 24 h with the indicated ligands. n = 6, except for 4OHT and Fulvestrant where n = 18. Data were analyzed by one-way ANOVA. Data are mean ± SEM.