体内分布
化学
成纤维细胞活化蛋白
体内
体外
聚乙二醇
放射化学
限制
生物化学
癌症
内科学
医学
生物
机械工程
生物技术
工程类
作者
Qing Ruan,Dajie Ding,L. Y. Diao,Junhong Feng,Guangxing Yin,Yuhao Jiang,Qianna Wang,Pei-jun Han,Jianyong Jiang,Junbo Zhang
标识
DOI:10.1021/acs.jmedchem.4c00031
摘要
Fibroblast activation protein (FAP), which is expressed on the cell membranes of fibroblasts in most solid tumors, has become an important target for tumor diagnosis and treatment. However, previously reported 99mTc-labeled FAPI-04 complexes have high blood uptake, limiting their use in the clinic. In this work, six 99mTc-labeled FAPI-46 derivatives with different linkers (different amino acids, peptides, or polyethylene glycol) were prepared and evaluated. They had good in vitro stability, hydrophilicity, and good specificity for FAP. The biodistribution and MicroSPECT images revealed that they all had high specific tumor uptake for FAP, and their blood uptake was significantly decreased. Among them, [99mTc]Tc-6–1 exhibited the highest target-to-nontarget ratios (tumor/blood: 6.06 ± 1.19; tumor/muscle: 10.26 ± 0.44) and good tumor uptake (16.15 ± 0.83%ID/g), which also had significantly high affinity for FAP, good in vivo stability, and safety. Therefore, [99mTc]Tc-6–1 holds great potential as a promising molecular tracer for FAP tumor imaging.
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