Abstract
Evasion of apoptosis is one of the hallmarks of cancer and any effective therapy primarily attempts to induce apoptosis. The evaluation of the degree of success of cancer therapy is currently mainly based on clinical and laboratory parameters and in a later stage on tumor shrinkage. However, none of these parameters provide an objective and early analysis of a therapeutic effect. Molecular imaging may provide a tool for this purpose by using not only pathophysiological but also biochemical effects of the therapy. First in the field, FDG-PET has been explored and demonstrated to offer insight in the amount of viable cells, even though false positives are commonly due to the lack of specificity of this particular radiopharmaceutical. More specific markers target the dying cells instead of those remaining alive. Specific apoptosis markers have been developed of which the radiolabeled Annexin A5 is the most intensely studied probe. Site-specific labeling strategies have improved this imaging probe with good results both in pre-clinical studies and in clinical trials, with promises for clinical applications. Caspase sensitive probes, such as the isatines, can also effectively image apoptosis but are limited due to the high background activities. More recent discoveries of small apoptosis sensitive probes, such as 18F-ML10, are currently being explored. In this review, the most important apoptosis sensitive probes are described from both a pre-clinical and a clinical perspective, highlighting their potential but also their limitations as an early marker for therapeutic success. It seems that apoptosis imaging can help to guide therapy, not by replacing the current methodology but by providing additional and useful information.
Keywords: Molecular imaging, apoptosis, early cancer therapy evaluation.
Current Pharmaceutical Design
Title:Molecular Imaging of Apoptosis for Early Prediction of Therapy Efficiency
Volume: 20 Issue: 14
Author(s): Marijke De Saint-Hubert, Matthias Bauwens and Felix M. Mottaghy
Affiliation:
Keywords: Molecular imaging, apoptosis, early cancer therapy evaluation.
Abstract: Evasion of apoptosis is one of the hallmarks of cancer and any effective therapy primarily attempts to induce apoptosis. The evaluation of the degree of success of cancer therapy is currently mainly based on clinical and laboratory parameters and in a later stage on tumor shrinkage. However, none of these parameters provide an objective and early analysis of a therapeutic effect. Molecular imaging may provide a tool for this purpose by using not only pathophysiological but also biochemical effects of the therapy. First in the field, FDG-PET has been explored and demonstrated to offer insight in the amount of viable cells, even though false positives are commonly due to the lack of specificity of this particular radiopharmaceutical. More specific markers target the dying cells instead of those remaining alive. Specific apoptosis markers have been developed of which the radiolabeled Annexin A5 is the most intensely studied probe. Site-specific labeling strategies have improved this imaging probe with good results both in pre-clinical studies and in clinical trials, with promises for clinical applications. Caspase sensitive probes, such as the isatines, can also effectively image apoptosis but are limited due to the high background activities. More recent discoveries of small apoptosis sensitive probes, such as 18F-ML10, are currently being explored. In this review, the most important apoptosis sensitive probes are described from both a pre-clinical and a clinical perspective, highlighting their potential but also their limitations as an early marker for therapeutic success. It seems that apoptosis imaging can help to guide therapy, not by replacing the current methodology but by providing additional and useful information.
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Cite this article as:
Saint-Hubert De Marijke, Bauwens Matthias and Mottaghy M. Felix, Molecular Imaging of Apoptosis for Early Prediction of Therapy Efficiency, Current Pharmaceutical Design 2014; 20 (14) . https://dx.doi.org/10.2174/13816128113196660664
DOI https://dx.doi.org/10.2174/13816128113196660664 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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