体内
化学
Pet成像
示踪剂
正电子发射断层摄影术
核医学
医学
生物
物理
生物技术
核物理学
作者
Huirong Li,Beibei Liang,Xiaoqing Gao,Ying Peng,Qingzhu Liu,Ling Qiu,Jianguo Lin
标识
DOI:10.1021/acs.molpharmaceut.3c01034
摘要
Cathepsin B, a lysosomal protease, is considered as a crucial biomarker for tumor diagnosis and treatment as it is overexpressed in numerous cancers. A stimulus-responsive SF scaffold has been reported to detect the activity of a variety of tumor-associated enzymes. In this work, a small-molecule PET tracer ([68Ga]NOTA-SF-CV) was developed by combining an SF scaffold with a cathepsin B-specific recognition substrate Cit-Val. Upon activation by cathepsin B, [68Ga]NOTA-SF-CV could form the cyclization product in a reduction environment, resulting in reduced hydrophilicity. This unique property could effectively prevent exocytosis of the tracer in cathepsin B-overexpressing tumor cells, leading to prolonged retention and amplified PET imaging signal. Moreover, [68Ga]NOTA-SF-CV had great targeting specificity to cathepsin B. In vivo microPET imaging results showed that [68Ga]NOTA-SF-CV was able to effectively visualize the expression level of cathepsin B in various tumors. Hence, [68Ga]NOTA-SF-CV may be served as a potential tracer for diagnosing cathepsin B-related diseases.
科研通智能强力驱动
Strongly Powered by AbleSci AI