Molecular Imaging of Apoptosis: The Case of Caspase-3 Radiotracers
Lucas Beroske1,2,3, Tim Van den Wyngaert1,2, Sigrid Stroobants1,2
1Molecular Imaging Center Antwerp, University of Antwerp, 2610 Wilrijk, Belgium.
Abstract:
The molecular imaging of apoptosis remains an important method for the diagnosis and monitoring of the progression of certain diseases and the evaluation of the efficacy of anticancer apoptosis-inducing therapies. Among the multiple biomarkers involved in apoptosis, activated caspase-3 is an attractive target, as it is the most abundant of the executioner caspases. Nuclear imaging is a good candidate, as it combines a high depth of tissue penetration and high sensitivity, features necessary to detect small changes in levels of apoptosis. However, designing a caspase-3 radiotracer comes with challenges, such as selectivity, cell permeability and transient caspase-3 activation. In this review, we discuss the different caspase-3 radiotracers for the imaging of apoptosis together with the challenges of the translation of various apoptosis-imaging strategies in clinical trials.
Insights
Molecular imaging of apoptosis using activated caspase-3 targets shows promise for disease diagnosis and cancer therapy evaluation. Challenges in developing effective caspase-3 radiotracers for nuclear imaging hinder clinical translation.
Area of Science:
- Molecular imaging
- Medical diagnostics
- Oncology
Background:
- Apoptosis imaging is crucial for disease monitoring and assessing cancer therapy effectiveness.
- Activated caspase-3 is a key executioner caspase and an attractive target for apoptosis imaging.
- Nuclear imaging offers high sensitivity and tissue penetration for detecting apoptosis.
Purpose of the Study:
- To review current caspase-3 radiotracers for apoptosis imaging.
- To discuss the challenges associated with developing and translating these radiotracers for clinical use.
Main Methods:
- Review of existing literature on caspase-3 radiotracers.
- Analysis of challenges in radiotracer design, including selectivity, cell permeability, and transient target activation.
Main Results:
- Activated caspase-3 is a viable target for molecular imaging of apoptosis.
- Several strategies for caspase-3 radiotracer development exist.
- Significant challenges remain in translating these imaging agents into clinical practice.
Conclusions:
- Caspase-3 radiotracers hold potential for advancing apoptosis imaging in disease diagnosis and cancer therapy.
- Overcoming challenges in radiotracer design and clinical translation is essential for realizing the full potential of this technology.


