PET小分子凋亡显像示踪剂的研究进展

Advances in small molecule radiotracer for PET imaging apoptosis

  • 摘要: 凋亡是细胞的程序化死亡过程。研究表明,小分子凋亡显像示踪剂可以帮助临床医师早期诊断疾病、检测疾病的进展、治疗后早期评估疗效、协助开发新的治疗方案、指导肿瘤个体化治疗。虽然临床上迫切期望一种理想的小分子凋亡显像PET示踪剂问世,但是一直未能实现,主要是因为临床应用的苛刻要求,包括对凋亡细胞的检测具有较高特异度和灵敏度、合理的生物学分布、药物的安全性、与放射性标记物的兼容性、常规PET设备的显像等。目前小分子凋亡显像PET示踪剂主要分为3类:显示凋亡蛋白活性的示踪剂、检测线粒体跨膜电位破坏的示踪剂和反应膜改变印记的示踪剂。

     

    Abstract: Apoptosis is a controlled program of cell death. So far, several studies have shown that small molecule apoptosis imaging tracers can help clinicians in early diagnosis of diseases, detection of disease development, early assessment of the efficacy of treatment and development of new treatment options. However, there is no ideal tracer of small molecule apoptosis imaging at present, the desirable small-molecule apoptosis imaging PET tracer should have the following characteristics:high specificity and sensitivity in detection of apoptotic cells, favorable biodistribution and safe profiles in vivo, compatible with radioactive markers and normal imaging of clinical PET. For different targets during apoptosis, currently, small molecule apoptosis imaging PET tracers are mainly divided into three categories:PET probes for caspase activation, PET probes for detection of collapse of mitochondrial membrane potential and PET probes for detection of apoptotic membrane imprint.

     

/

返回文章
返回