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Updated: Aug 7, 2026

An In Vitro Approach to Photodynamic Therapy
Published on: August 17, 2018
Photodynamic therapy agent with a built-in apoptosis sensor for evaluating its own therapeutic outcome in situ
Klara Stefflova1, Juan Chen, Diane Marotta
1Department of Chemistry, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA.
Abstract:
Identifying the extent of apoptosis in cells or tissues after cancer therapy in real time would be a powerful firsthand tool for assessing therapeutic outcome. We combined therapeutic and imaging functions in one agent, choosing photodynamic therapy (PDT) as an appropriate cancer treatment modality. This agent induces photodamage in irradiated cells and simultaneously identifies apoptotic cells by near-infrared fluorescence. This photodynamic therapy agent with a built-in apoptosis sensor (PDT-BIAS) contains a fluorescent photosensitizer used as an anticancer drug, connected to a fluorescence quencher by a caspase-3 cleavable peptide linker. We demonstrated that cleavage of the peptide linker by caspase-3, one of the executioner caspases involved in apoptosis, results in a detectable increase of fluorescence in solution and in cancer cells after PDT treatment. The apoptosis involvement and drug effectiveness were confirmed by Apoptag and cell viability (MTT) assays supporting the ability of PDT-BIAS to induce and image apoptosis in situ.
Insights
We developed a novel agent that combines photodynamic therapy (PDT) with an apoptosis sensor. This agent, PDT-BIAS, treats cancer and simultaneously images apoptosis in real-time, aiding therapeutic outcome assessment.
Area of Science:
- Oncology
- Biochemistry
- Medical Imaging
Background:
- Real-time assessment of apoptosis post-cancer therapy is crucial for evaluating treatment efficacy.
- Photodynamic therapy (PDT) is an effective cancer treatment modality.
- Current methods for apoptosis detection can be time-consuming and lack real-time imaging capabilities.
Purpose of the Study:
- To develop a single-agent system that combines photodynamic therapy with in situ apoptosis imaging.
- To create a tool for real-time monitoring of therapeutic outcomes in cancer treatment.
Main Methods:
- Development of a "photodynamic therapy agent with a built-in apoptosis sensor" (PDT-BIAS).
- PDT-BIAS incorporates a fluorescent photosensitizer linked to a quencher via a caspase-3 cleavable peptide.
- In vitro experiments utilizing cancer cells, Apoptag, and MTT assays to validate functionality.
Main Results:
- Cleavage of the peptide linker by caspase-3 upon apoptosis induction resulted in a measurable increase in fluorescence.
- PDT-BIAS successfully induced and imaged apoptosis in cancer cells following PDT treatment.
- Apoptosis involvement and drug efficacy were confirmed by complementary assays.
Conclusions:
- PDT-BIAS effectively combines cancer therapy and apoptosis imaging in a single agent.
- This novel agent enables real-time, in situ monitoring of apoptosis, facilitating prompt assessment of therapeutic response.
- PDT-BIAS holds promise for improving cancer treatment monitoring and personalized medicine approaches.
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