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Published on: March 17, 2023
Recent Advances in the Enzyme-Activatable Organic Fluorescent Probes for Tumor Imaging and Therapy
Song-Bo Lu1, Luyao Wei1, Wenjing He1
1Shenzhen Key Laboratory of Smart Healthcare Engineering Guangdong Provincial Key Laboratory of Advanced Biomaterials Department of Biomedical Engineering, Southern University of Science and Technology (SUSTech), Shenzhen, 518055, P. R. China.
Abstract:
The exploration of advanced probes for cancer diagnosis and treatment is of high importance in fundamental research and clinical practice. In comparison with the traditional "always-on" probes, the emerging activatable probes enjoy advantages in promoted accuracy for tumor theranostics by specifically releasing or activating fluorophores at the targeting sites. The main designing principle for these probes is to incorporate responsive groups that can specifically react with the biomarkers (e. g., enzymes) involved in tumorigenesis and progression, realizing the controlled activation in tumors. In this review, we summarize the latest advances in the molecular design and biomedical application of enzyme-responsive organic fluorescent probes. Particularly, the fluorophores can be endowed with ability of generating reactive oxygen species (ROS) to afford the photosensitizers, highlighting the potential of these probes in simultaneous tumor imaging and therapy with rational design. We hope that this review could inspire more research interests in the development of tumor-targeting theranostic probes for advanced biological studies.
Insights
Activatable probes offer improved accuracy for cancer theranostics by targeting tumor biomarkers. These enzyme-responsive organic fluorescent probes enable simultaneous imaging and treatment via reactive oxygen species generation.
Area of Science:
- Biomedical Engineering
- Organic Chemistry
- Oncology
Background:
- Advanced probes are crucial for accurate cancer diagnosis and treatment.
- Activatable probes offer superior tumor theranostics compared to traditional always-on probes.
- Enzyme-responsive probes enable targeted activation of fluorophores at tumor sites.
Purpose of the Study:
- To review recent advancements in molecular design and biomedical applications of enzyme-responsive organic fluorescent probes.
- To highlight the potential of these probes in simultaneous tumor imaging and therapy.
- To inspire further research in tumor-targeting theranostic probes.
Main Methods:
- Incorporation of responsive groups that react with tumor-specific biomarkers (e.g., enzymes).
- Design of fluorophores capable of generating reactive oxygen species (ROS) for photodynamic therapy.
- Summarization of latest research on molecular design and biomedical applications.
Main Results:
- Enzyme-responsive probes demonstrate controlled activation in tumors.
- Fluorophores can be engineered as photosensitizers for ROS generation.
- Rational probe design facilitates simultaneous tumor imaging and therapy.
Conclusions:
- Enzyme-responsive organic fluorescent probes represent a significant advancement in cancer theranostics.
- These probes enhance diagnostic accuracy and therapeutic efficacy through targeted activation.
- Future development holds promise for improved tumor-targeting theranostic strategies.

