Biological approaches were pursued to inhibit CREB function in breast cancer cells such as the utilization of dominant‐negative CREB mutants, CREB “decoy” oligonucleotides and RNA interference.38, 39, 40, 41 However, clinical applications of these approaches are rather limited since gene therapy techniques would also be required.42 Therefore, utilizing small organic molecules to prevent breast cancer‐induced bone metastasis and osteolysis could be of great interest due to their better pharmacokinetic properties. Here, CREB1 is linked to breast cancer.