凋亡的分子成像仍然是诊断和监测某些疾病的进展以及评估抗癌凋亡诱导疗法功效的重要方法。在参与细胞凋亡的多种生物标志物中,激活的caspase-3是一个有吸引力的目标,因为它是execution子中最丰富的caspases。核成像是一个很好的候选人,因为它结合了高组织穿透深度和高灵敏度,检测细胞凋亡水平微小变化所必需的特征。然而,设计caspase-3放射性示踪剂面临挑战,如选择性,细胞通透性和瞬时caspase-3激活。在这次审查中,我们讨论了用于细胞凋亡成像的不同caspase-3放射性示踪剂,以及临床试验中各种细胞凋亡成像策略翻译的挑战。
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.