An activatable endoplasmic reticulum-targeted probe for NIR imaging-guided photothermal therapy

Area of Science:

• Biomedical Engineering
• Chemical Biology
• Cancer Research

Background:

• Hydrogen peroxide (H₂O₂) is a key signaling molecule implicated in various cellular processes and diseases, including cancer.
• Targeted delivery of therapeutic agents to specific cellular compartments like the endoplasmic reticulum is crucial for effective cancer treatment.
• Theranostic probes offer simultaneous diagnostic and therapeutic capabilities, improving treatment efficacy and monitoring.

Purpose of the Study:

• To develop a novel theranostic probe activated by hydrogen peroxide (H₂O₂).
• To achieve specific targeting of the endoplasmic reticulum in cancer cells overexpressing H₂O₂.
• To enable simultaneous detection via fluorescence and therapeutic intervention via photothermal therapy.

Main Methods:

• Design and synthesis of an H₂O₂-activated probe.
• Endoplasmic reticulum targeting moiety incorporation.
• Evaluation of probe activation by H₂O₂, leading to enhanced near-infrared (NIR) fluorescence and photothermal signals.
• Assessment of cancer cell recognition and photothermal therapy efficacy in vitro.

Main Results:

• The developed probe demonstrated H₂O₂-triggered activation.
• Activation resulted in significantly increased NIR fluorescence and photothermal signals.
• The probe specifically recognized and localized within the endoplasmic reticulum of H₂O₂-overexpressing cancer cells.
• Effective photothermal therapy was achieved in the targeted endoplasmic reticulum environment.

Conclusions:

• A novel H₂O₂-activated, endoplasmic reticulum-targeted theranostic probe was successfully developed.
• The probe enables specific H₂O₂ detection and targeted photothermal therapy in cancer cells.
• This theranostic strategy holds promise for improved cancer diagnosis and treatment by targeting the endoplasmic reticulum.