2. Academic Validation
  3. A Nitroreductase-Responsive Type I Photosensitizer with Aggregation-Induced Emission Characteristics for Precise Hypoxic Cancer Theranostics

A Nitroreductase-Responsive Type I Photosensitizer with Aggregation-Induced Emission Characteristics for Precise Hypoxic Cancer Theranostics

  • ACS Nano. 2025 Jul 15;19(27):24701-24712. doi: 10.1021/acsnano.4c16139.
Kristy W K Lam 1,  Yaojia Zhang 2,  Wutong Du 1,  Jie Sun 2,  Feiyi Sun 1 3,  Yuyang Chen 1 4,  Charlie C H Ma 1,  Jacky W Y Lam 1 5,  Ryan T K Kwok 1 5,  Jianwei Sun 1,  Xuewen He 2,  Ben Zhong Tang 1 6
Affiliations

Affiliations

  • 1 Department of Chemistry, Department of Chemical and Biological Engineering, Hong Kong Branch of Chinese National Engineering Research Center for Tissue Restoration and Reconstruction, and State Key Laboratory of Nervous System Disorders, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong 999077, China.
  • 2 The Key Lab of Health Chemistry and Molecular Diagnosis of Suzhou, College of Chemistry, Chemical Engineering and Materials Science, Soochow University, 199 Ren'ai Road, Suzhou, Jiangsu 215123, China.
  • 3 Ph.D.Department of Comprehensive Basic Experiment, The Ninth Medical Center. of Chinese PLA General Hospital, Beijing 100101, P.R. of China.
  • 4 Institute of Infectious Diseases, Shenzhen Bay Laboratory. Shenzhen 518132, China.
  • 5 HKUST-Shenzhen Research Institute, No. 9 Yuexing first RD, South Area Hi-Tech Park, Nanshan, Shenzhen 518057, China.
  • 6 School of Science and Engineering, Shenzhen Institute of Aggregate Science and Technology, The Chinese University of Hong Kong, Shenzhen, Shenzhen , Guangdong518172, China.
PMID: 40605741 DOI: 10.1021/acsnano.4c16139
Abstract

Cancer remains a significant global health challenge, with early and accurate detection being key to improving treatment outcomes. Developing targeted photosensitizers (PS) that selectively image and treat Cancer cells is critical for Cancer diagnosis, staging, and treatment monitoring. Understanding the hypoxic nature of solid tumors is essential in Cancer detection, as hypoxia is associated with tumor aggressiveness and therapy resistance. Nitroreductase (NTR), which is overexpressed in hypoxic tumors, offers a target for selective imaging and treatment. In this study, we developed a type-I PS called TPAPyN, which is responsive to NTR. TPAPyN facilitates the imaging of hypoxic Cancer cells and facilitates image-guided photodynamic therapy (PDT). Because of photoinduced electron transfer, TPAPyN does not emit fluorescence in the aqueous environment. However, its fluorescence is restored when NTR cleaves the nitrofuran quencher, forming highly emissive TPAPy aggregates. This characteristic makes TPAPyN a valuable fluorescent probe for specific imaging of NTR-overexpressed Cancer cells. Additionally, TPAPy exhibits high efficiency in generating Reactive Oxygen Species, indicating its potential as a PS for Cancer treatment via PDT.

Keywords

aggregation-induced emission; hypoxia; image-guided photodynamic therapy; nitroreductase; reactive oxygen species.

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