Establishment of nuclear receptor-mediated assay for sex-steroid like compounds

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Steroid hormones exert their actons through cognate nuclear receptors, which act ligand-inducible transcriptional factors. For this ligand-induced transactivation, ligand-bound nuclear receptors, nuclear receptors depend on ligand binding, but it is induced only by agonist, but not antgonist. In the present study, we searched novel coactivators for nuclear receptors for estrogen, androgen mineralcorticoid, vitamin D by biochemical approaches and yeast two-hybrid system, and found several candidate cDNAs. Especially, we found that p68/p72 acts as a co-activator specific for ERα. Moreover, we developed an assay system based on the interactions of coactivators with nuclear receptors in yeast to evaluate agonistic/antagonistid activity of related compounds.