FXXLF Proteomimetics of Coactivator Proteins Binding to the Androgen Receptor

A series of novel substituted biphenyl compounds was designed as alpha helical proteomimetics with the aim of inhibiting the binding of coactivator proteins to the nuclear hormone receptor coactivator binding pocket. The final products were evaluated using estrogen receptor reporter gene assays and competitive binding assays to demonstrate their effectiveness as competitive binding inhibitors. The results from this study indicate that these proteomimetics possess the ability to inhibit this protein-protein interaction.