Molecular Imaging Center Antwerp, University of Antwerp, 2610 Wilrijk, Belgium.
Department of Nuclear Medicine, Antwerp University Hospital, 2650 Edegem, Belgium.
Int J Mol Sci. 2021 Apr 11;22(8):3948. doi: 10.3390/ijms22083948.
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.
细胞凋亡的分子成像仍然是诊断和监测某些疾病进展以及评估抗癌细胞凋亡诱导治疗效果的重要方法。在涉及细胞凋亡的多种生物标志物中，活化的半胱氨酸蛋白酶-3（caspase-3）是一个很有吸引力的靶点，因为它是效应半胱氨酸蛋白酶中含量最丰富的一种。核成像技术是一个很好的候选方法，因为它结合了高组织穿透深度和高灵敏度，这是检测细胞凋亡水平微小变化所必需的。然而，设计半胱氨酸蛋白酶-3放射性示踪剂存在一些挑战，如选择性、细胞通透性和半胱氨酸蛋白酶-3的短暂激活。在这篇综述中，我们讨论了用于细胞凋亡成像的不同半胱氨酸蛋白酶-3放射性示踪剂，以及将各种细胞凋亡成像策略转化为临床试验所面临的挑战。
