Tumor Stimulus-Activatable Pretheranostic Agent: One Key to Three Locks.

Area of Science:

• Biomedical Engineering
• Materials Science
• Oncology

Background:

• Uncontrolled distribution of antitumor agents hinders effective cancer theranostics.
• Development of tumor-specific systems is crucial for improving therapeutic specificity and efficiency.

Purpose of the Study:

• To design and synthesize tumor stimulus-activatable pretheranostic agents for enhanced cancer theranostics.
• To create a general platform using triphenylamine derivatives for targeted tumor detection and treatment.

Main Methods:

• Synthesized triphenylamine derivatives (TPA-2T-FSQ, TPA-2T-BSZ, TPA-2T-ML) with specific identifying groups for hypochlorite (HClO).
• Investigated the oxidation of the sulfur atom in phenothiazine by HClO and its effect on electronic properties.
• Utilized the overexpressed HClO in tumors to trigger multimodal signals (NIR fluorescence, photothermal, photoacoustic).

Main Results:

• TPA-2T-FSQ demonstrated efficient oxidation by HClO, leading to a significant redshift in absorbance and emission wavelengths.
• The developed system successfully activated NIR fluorescence, photothermal, and photoacoustic signals in response to tumor-specific HClO.
• The agent enabled multimodal diagnosis and treatment of tumors, showcasing its theranostic potential.

Conclusions:

• A general design for tumor stimulus-triggerable pretheranostic agents was successfully established.
• The TPA-2T-FSQ agent offers improved theranostic accuracy and efficiency by leveraging tumor-specific hypochlorite.
• This approach represents a promising strategy for precision medicine in cancer treatment.