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Molecular Imaging of Apoptosis: The Case of Caspase-3 Radiotracers
Authors:Lucas Beroske  Tim Van den Wyngaert  Sigrid Stroobants  Pieter Van der Veken  Filipe Elvas
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;
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.
Keywords:caspase-3  radiotracer  activity-based probe  substrate-based probe  positron emission tomography  single-photon emission computed tomography
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