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Past, present, and future of annexin A5: from protein discovery to clinical applications
Hendrikus H Boersma1, Bas L J H Kietselaer, Leo M L Stolk
1Department of Nuclear Medicine, Maastricht University Hospital, Maastricht, The Netherlands. hboe@kfls.azm.nl
Abstract:
In this article, we review the clinical aspects of imaging with the programmed cell-detecting protein annexin A5 (anxA5). AnxA5 binds to phosphatidylserine, which is one of the "eat me" signals at the surface of the apoptotic cell. This biologic property forms the basis for the development of anxA5 as a diagnostic tool. Within this context, the clinical relevance, limitations, and future perspectives of this approach of visualizing cell death are discussed in this article, as are other potential applications of anxA5. Furthermore, the biologic properties and the radiopharmaceutical, pharmacologic, and biodistribution aspects of anxA5 are reviewed and discussed in this article. Radiolabeled anxA5 bears the promise of becoming a clinically applied radiopharmaceutical with potential applications in cardiology and oncology. Visualization of cell death is important in pathologies such as myocardial infarction, atherosclerosis, and cancer. Furthermore, radiolabeled anxA5 may be developed as a tool for monitoring cell death-inducing or cell death-preventing therapies. In addition, experiences with radiolabeled anxA5 open novel avenues for drug targeting with anxA5 as a biologic "cruise missile."
Insights
Annexin A5 (anxA5) imaging visualizes cell death by binding to apoptotic cells. This diagnostic tool shows promise in cardiology and oncology for disease detection and therapy monitoring.
Area of Science:
- Biomedical Imaging
- Molecular Diagnostics
- Cell Biology
Background:
- Annexin A5 (anxA5) targets phosphatidylserine, an 'eat me' signal on apoptotic cells.
- This interaction forms the basis for anxA5 as a diagnostic imaging agent.
- Visualizing cell death is crucial for understanding pathologies like myocardial infarction, atherosclerosis, and cancer.
Purpose of the Study:
- To review the clinical applications of annexin A5 imaging.
- To discuss the biologic properties, radiopharmaceutical aspects, and biodistribution of anxA5.
- To explore the potential of anxA5 in diagnostics, therapy monitoring, and drug targeting.
Main Methods:
- Review of clinical data and research on annexin A5 imaging.
- Analysis of anxA5's biologic properties and radiopharmaceutical characteristics.
- Discussion of potential applications in various medical fields.
Main Results:
- Radiolabeled anxA5 demonstrates potential as a clinical radiopharmaceutical.
- AnxA5 imaging can visualize cell death in conditions like myocardial infarction, atherosclerosis, and cancer.
- AnxA5 holds promise for monitoring therapies and as a platform for targeted drug delivery.
Conclusions:
- Annexin A5 imaging is a promising diagnostic tool for visualizing cell death.
- Its applications extend to cardiology, oncology, and monitoring therapeutic interventions.
- AnxA5 offers novel opportunities for targeted drug delivery strategies.

