PRI-724, a small molecule specific inhibitor of the β-catenin/CREB-binding protein (CBP) interaction, selectively disrupts the interaction between β-catenin and represses a subset of TCF/b-catenin-mediated transcription and has demonstrated safety and efficacy in multiple clinical trials targeting various cancers [NCT01606579, NCT01764477]. The gene discussed is CREBBP; the disease is cancer.