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

• Published in: Angewandte Chemie International Edition Vol. 61; no. 15; pp. e202114600 - n/a
• Main Authors: Wang, Kang‐Nan, Liu, Liu‐Yi, Mao, Duo, Hou, Ming‐Xuan, Tan, Cai‐Ping, Mao, Zong‐Wan, Liu, Bin
• Format: Journal Article
• Language: English
• Published: Germany Wiley Subscription Services, Inc 04.04.2022
• Edition: International ed. in English
• Subjects: Ablation; Cancer; Cell cycle; Cell Cycle Checkpoints; Cell proliferation; Drug Delivery Systems; Histone Deacetylase Inhibition; Histones; Humans; Neoplasms - drug therapy; Nuclear Targeting; Nuclei (cytology); Nucleic Acid Damage; Nucleic acids; Photochemotherapy; Photodynamic therapy; Photosensitization; Photosensitizer; Photosensitizing Agents - pharmacology; Photosensitizing Agents - therapeutic use; Telomerase Inhibition; Telomeres; Tumors; Histone Deacetylase Inhibition; Nucleic Acid Damage; Telomerase Inhibition; Nuclear Targeting; Photosensitizer
• ISSN: 1433-7851; 1521-3773; 1521-3773
• DOI: 10.1002/anie.202114600

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. A nuclear‐targeted material MeTPAE with AIE characteristics was developed. MeTPAE can not only interact with HDACs to inhibit cell proliferation, but also damage telomere and nucleic acids precisely through photodynamic treatment. The cocktail strategy of MeTPAE caused obvious cell cycle arrest and showed excellent photodynamic therapy (PDT) anti‐tumor activity, which offered new opportunities for the effective treatment of malignant tumors.