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. 2013 Jun 3;288(29):21105–21116. doi: 10.1074/jbc.M113.463455

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© 2013 by The American Society for Biochemistry and Molecular Biology, Inc.

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FIGURE 8. — The effect of SERMs on AF2ER, AF2ERΔF, AF2ER-L511R, and ERαΔH12 activities. A, HepG2 cells were cotransfected with 3xERE-TATA-luc, pRL-TK, and the expression vector for AF2ER, AF2ERΔF, AF2ER-L511R, ΔH12, or pcDNA3 and then treated with either vehicle (Veh), 10 nm E2, ICI, OHT, or Ral. The luciferase activity is represented as fold change against the empty expression vector (pcDNA3) in the presence of each ligand. Luciferase activity is represented as mean ± S.D. a, b, and c, p < 0.001 against the vehicle level of each receptor. B, HepG2 cells were cotransfected with pG5-luc and the following combinations: pBIND-LBD/AF2ER in the presence of pACT or pACT-LBD/AF2ER, pBIND-LBD/AF2ERΔF in the presence of pACT or pACT-LBD/AF2ERΔF, pBIND-LBD/AF2ER-L511R in the presence of pACT or pACT-LBD/AF2ER-L511R, and pBIND-LBD/ΔH12 in the presence of pACT or pACT-LBD/ΔH12. Cells were treated with either vehicle, 10 nm E2, ICI, OHT, or Ral. The luciferase activity is represented as a fold change over vehicle in each pACT and pBIND-LBD co-transfected sample. Luciferase activity is represented as mean ± S.D. a, c, and e, p < 0.001 against vehicle in each pACT and pBIND-LBD co-transfected sample; b, d, and f, p < 0.001 against vehicle in each pACT-LBD and pBIND-LBD co-transfected sample.