Fig. 5.

Cooperative activation by agonist and antagonist requires receptor dimer to bind to DNA. HepG2 (A) and HeLa (B) cells cotransfected with 1/2ERE-Luc or EGRE-Luc reporter genes as well as the indicated ER expression vectors were treated with vehicle (0.1% ethanol), 100 nM CE, 10 nM BAZ, or 100 nM CE + 10 nM BAZ for 24 hours. Data are presented as relative luciferase activity compared to EGRE-Luc plus ERα-G521R + ERα(GSCKV) cotransfected samples treated with 100 nM CE + 10 nM BAZ. Values represent the average ± S.E.M. of three independent experiments.