Development of [18F]ICMT-11 for Imaging Caspase-3/7 Activity during Therapy-Induced Apoptosis
Segundo Francisco García-Argüello1,2, Beatriz Lopez-Lorenzo3,4, Bart Cornelissen5
1Centro de Investigaciones Médico-Sanitarias, Fundación General Universidad de Málaga, 29010 Málaga, Spain.
Abstract:
Insufficient apoptosis is a recognised hallmark of cancer. A strategy to quantitatively measure apoptosis in vivo would be of immense value in both drug discovery and routine patient management. The first irreversible step in the apoptosis cascade is activation of the "executioner" caspase-3 enzyme to commence cleavage of key structural proteins. One strategy to measure caspase-3 activity is Positron Emission Tomography using isatin-5-sulfonamide radiotracers. One such radiotracer is [18F]ICMT-11, which has progressed to clinical application. This review summarises the design and development process for [18F]ICMT-11, suggesting potential avenues for further innovation.
Insights
Measuring cancer cell death (apoptosis) in vivo is crucial. [18F]ICMT-11, a novel radiotracer, enables quantitative positron emission tomography imaging of caspase-3 activity, aiding cancer drug discovery and patient care.
Area of Science:
- Biomedical Imaging
- Oncology
- Molecular Biology
Background:
- Insufficient apoptosis is a key characteristic of cancer.
- Quantitative in vivo apoptosis measurement is vital for cancer drug discovery and patient management.
- Caspase-3 activation is an early, irreversible step in apoptosis.
Purpose of the Study:
- To review the design and development of [18F]ICMT-11, a positron emission tomography radiotracer for measuring caspase-3 activity.
- To highlight the clinical progression of [18F]ICMT-11.
- To suggest future innovations in apoptosis imaging.
Main Methods:
- Development of isatin-5-sulfonamide-based radiotracers.
- Utilizing Positron Emission Tomography (PET) for imaging.
- Focus on quantitative measurement of caspase-3 activity in vivo.
Main Results:
- [18F]ICMT-11 has been successfully developed as a radiotracer for caspase-3 imaging.
- The radiotracer has progressed to clinical application.
- The review details the design and development pathway.
Conclusions:
- [18F]ICMT-11 represents a significant advancement in quantitative apoptosis imaging.
- This technology holds promise for improving cancer diagnostics and therapeutic strategies.
- Further innovation in radiotracer design could enhance clinical utility.
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