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Published on: September 3, 2013
Activatable dual-functional molecular agents for imaging-guided cancer therapy
Peng Zhang1, Yaowei Zhu2, Chunsheng Xiao3
1Key Laboratory of Polymer Ecomaterials, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, PR China; Jilin Biomedical Polymers Engineering Laboratory, Changchun 130022, PR China; State Key Laboratory of Molecular Engineering of Polymers (Fudan University), Shanghai 200433, PR China.
Abstract:
Theranostics has attracted great attention due to its ability to combine the real-time diagnosis of cancers with efficient treatment modalities. Activatable dual-functional molecular agents could be synthesized by covalently conjugating imaging agents, therapeutic agents, stimuli-responsive linkers and/or targeting molecules together. They could be selectively activated by overexpressed physiological stimuli or external triggers at the tumor sites to release imaging agents and cytotoxic drugs, thus offering many advantages for tumor imaging and therapy, such as a high signal-to-noise ratio, low systemic toxicity, and improved therapeutic effects. This review summarizes the recent advances of dual-functional molecular agents that respond to various physiological or external stimuli for cancer theranostics. The molecular designs, synthetic strategies, activatable mechanisms, and biomedical applications of these molecular agents are elaborated, followed by a brief discussion of the challenges and opportunities in this field.
Insights
Activatable dual-functional molecular agents offer advanced cancer theranostics by combining real-time diagnosis and targeted treatment. These agents release imaging and therapeutic payloads specifically at tumor sites, enhancing efficacy and reducing side effects.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Oncology
Background:
- Theranostics integrates diagnosis and therapy for improved cancer management.
- Activatable dual-functional molecular agents offer precise, stimulus-responsive cancer care.
- These agents combine imaging and therapeutic functionalities for targeted delivery.
Purpose of the Study:
- To review recent advances in stimuli-responsive dual-functional molecular agents for cancer theranostics.
- To elaborate on the design, synthesis, and activation mechanisms of these agents.
- To discuss their biomedical applications, challenges, and future opportunities.
Main Methods:
- Review of recent scientific literature on dual-functional molecular agents for cancer theranostics.
- Analysis of molecular designs, synthetic strategies, and stimuli-responsive mechanisms.
- Evaluation of biomedical applications and performance in preclinical and clinical studies.
Main Results:
- Dual-functional agents can be designed to respond to various physiological or external stimuli.
- Stimuli-responsive activation enables targeted release of imaging and therapeutic agents at tumor sites.
- These agents demonstrate advantages such as high signal-to-noise ratio, low systemic toxicity, and improved therapeutic effects.
Conclusions:
- Stimuli-responsive dual-functional molecular agents represent a promising strategy for advanced cancer theranostics.
- Further research into molecular design and activation mechanisms can optimize their clinical translation.
- Addressing current challenges will unlock the full potential of these agents in personalized cancer treatment.

