A Nuclear-Targeted AIE Photosensitizer for Enzyme Inhibition and Photosensitization in Cancer Cell Ablation

The nucleus is considered the ideal target for anti-tumor therapy because DNA and some enzymes in the nucleus are the main causes of cell canceration and malignant proliferation. However, nuclear target drugs with good biosafety and high efficiency in cancer treatment are rare. Herein, a nuclear-targeted material MeTPAE with aggregation-induced emission (AIE) characteristics was developed based on a triphenylamine structure skeleton. MeTPAE can not only interact with histone deacetylases (HDACs) to inhibit cell proliferation but also damage telomere and nucleic acids precisely through photodynamic treatment (PDT). The cocktail strategy of MeTPAE caused obvious cell cycle arrest and showed excellent PDT anti-tumor activity, which offered new opportunities for the effective treatment of malignant tumors.

Automated summary

The nucleus is considered an ideal target for anti-tumor therapy, but there is currently a lack of nuclear-targeted drugs with good biosafety and high efficacy. In this study, a new nuclear-targeted material MeTPAE was developed, which can interact with HDACs to inhibit cell proliferation and precisely damage the nucleus through PDT. This strategy caused cell cycle arrest and exhibited excellent anti-tumor activity.