Molecular Imaging of Apoptosis: The Case of Caspase-3 Radiotracers

被引:87
作者
Beroske, Lucas [1 ,2 ,3 ]
Van den Wyngaert, Tim [1 ,2 ]
Stroobants, Sigrid [1 ,2 ]
Van der Veken, Pieter [3 ]
Elvas, Filipe [1 ,2 ]
机构
[1] Univ Antwerp, Mol Imaging Ctr Antwerp, B-2610 Antwerp, Belgium
[2] Antwerp Univ Hosp, Dept Nucl Med, B-2650 Edegem, Belgium
[3] Univ Antwerp, Lab Med Chem, B-2610 Antwerp, Belgium
关键词
caspase-3; radiotracer; activity-based probe; substrate-based probe; positron emission tomography; single-photon emission computed tomography; INDUCED TUMOR APOPTOSIS; ACTIVITY-BASED PROBES; IN-VIVO EVALUATION; SELECTIVE DETECTION; TREATMENT RESPONSE; PET TRACER; DESIGN; CANCER; DERIVATIVES; ACTIVATION;
D O I
10.3390/ijms22083948
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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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页数:19
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