Molecular Imaging of Apoptosis: The Case of Caspase-3 Radiotracers |
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Authors: | Lucas Beroske Tim Van den Wyngaert Sigrid Stroobants Pieter Van der Veken Filipe Elvas |
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Affiliation: | 1.Molecular Imaging Center Antwerp, University of Antwerp, 2610 Wilrijk, Belgium; (L.B.); (T.V.d.W.); (S.S.);2.Department of Nuclear Medicine, Antwerp University Hospital, 2650 Edegem, Belgium;3.Laboratory of Medicinal Chemistry, University of Antwerp, 2610 Wilrijk, Belgium; |
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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. |
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Keywords: | caspase-3 radiotracer activity-based probe substrate-based probe positron emission tomography single-photon emission computed tomography |
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