Molecular Imaging of Apoptosis In Vivo with Scintigraphic and Optical Biomarkers – A Status Report

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 17, 14 Issues, 2017

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
Université Clermont Auvergne

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Molecular Imaging of Apoptosis In Vivo with Scintigraphic and Optical Biomarkers – A Status Report

Anti-Cancer Agents in Medicinal Chemistry, 9(9): 968-985.

Author(s): Andreas Faust, Sven Hermann, Stefan Wagner, Gunther Haufe, Otmar Schober, Michael Schafers and Klaus Kopka.

Affiliation: Department of Nuclear Medicine, University Hospital Munster, Albert-Schweitzer-Str. 33, D-48149 Munster, Germany.


The balance between proliferation and programmed cell death – apoptosis – is essential for multicellular organisms which use apoptosis to regulate and maintain the number and type of their cells during embryogenesis, growth and homeostasis. Increased cell proliferation or enhanced cell loss can be caused by dysregulated apoptosis and are observed in various diseases: in clinical scenarios such as neurodegenerative disorders, myocardial infarction and stroke the rate of apoptosis is upregulated compared to the physiological situation, while in clinical scenarios such as cancer or autoimmune diseases which are connected with pathological proliferation, apoptosis is often downregulated. Therefore, non-invasive imaging of apoptosis is of great clinical interest as patients would clearly benefit from the diagnosis of cell loss post infarction or from monitoring apoptosis triggered by chemotherapy or radiation therapy of tumours. Several biochemical transformations occur in apoptotic cells offering different biological targets for the development of specific molecular biomarkers of apoptosis. Key steps that occur during apoptosis have already been evaluated; among these are the externalisation of phospholipid phosphatidylserine to the outer leaflet of the cell membrane, which can be visualized by labeled annexin A5 and the activation of caspases, especially effector caspase-3, which can be addressed by labeled enzyme substrates or synthetic caspase inhibitors. Here, recent advances in tracer development for the molecular imaging techniques PET, SPECT and optical imaging are presented, the discussion of breakthroughs is involved, drawbacks and methodological issues of apoptosis imaging are highlighted.


Molecular imaging, positron emission tomography PET, single photon emission computed tomography SPECT, targeted ligands, optical imaging, annexin A5, inhibitors of caspases, dansyl derived agents.

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Article Details

Volume: 9
Issue Number: 9
First Page: 968
Last Page: 985
Page Count: 18
DOI: 10.2174/187152009789377754
Price: $58

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