Proteolytic targeting chimera (PROTAC) methodology is promising for cancer therapy but limited by the insufficient distribution and accumulation in most tumors. Here the authors assemble Ce6 and mitochondrial-targeting peptide into PROTAC agent dBET6 to achieve enhanced accumulation in tumor cells and subsequent BRD4 degradation, apoptosis induction thereby elicit its anti-cancer treatment.
- Fan Tong
- Yufan Wang
- Huile Gao