Example 11
To examine the inhibitory activity of brilacidin on PDE4 phosphodiesterase, inhibition assays of PDE4 were performed using brilacidin. The PDE-Glo phosphodiesterase assay (Promega, Madison, Wis.) was performed using 8 ng of PDE4B3, 1 μM cAMP substrate and brilacidin. The compounds and PDE4B (BPS Biosciences, San Diego, Calif.) were mixed and pre-incubated at room temperature for 15 minutes. Substrate was added and the reaction was incubated for 10 minutes at room temperature. Data are presented as luminescence units (RLU). Brilacidin inhibited PDE4 in a dose dependent manner with an IC50 in the 3 μM range (