Transforming a Targeted Porphyrin Theranostic Agent into a PET Imaging Probe for Cancer.
Transforming a Targeted Porphyrin Theranostic Agent into a PET Imaging Probe for Cancer.
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DOI：
10.7150/thno/v01p0363
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发表时间：
2011
期刊：
影响因子：
12.4
通讯作者：
Zheng G
中科院分区：
文献类型：
--
作者：
Shi J;Liu TW;Chen J;Green D;Jaffray D;Wilson BC;Wang F;Zheng G
基于卟啉的光敏剂是用于癌症的光动力疗法（PDT）和荧光成像的有用试剂。卟啉也是优良的金属螯合剂，形成高度稳定的金属络合物，使其成为放射性同位素的有效递送载体。在这里，我们研究了将64 Cu纳入卟啉-肽-叶酸（PPF）探针先前开发的叶酸受体（FR）靶向荧光/PDT剂的可能性，并评估了将所得的64 Cu-PPF转化为正电子发射断层扫描（PET）探针用于癌症成像的潜力。非侵入性PET成像，然后放射性测定评价肿瘤蓄积，64 Cu-PPF的药代动力学和生物分布。FR阳性肿瘤中的64 Cu-PPF摄取在小动物PET图像上可见，24 h后观察到较高的肿瘤/肌肉比（8.88 ± 3.60）。竞争性阻断研究证实了FR介导的示踪剂被肿瘤摄取。PPF易于进行有效的64 Cu放射性标记，同时保持其良好的生物分布、药代动力学和选择性肿瘤摄取，这为将肿瘤靶向卟啉类光敏剂转化为PET成像探针提供了一种稳健的策略。
Porphyrin based photosensitizers are useful agents for photodynamic therapy (PDT) and fluorescence imaging of cancer. Porphyrins are also excellent metal chelators forming highly stable metallo-complexes making them efficient delivery vehicles for radioisotopes. Here we investigated the possibility of incorporating 64Cu into a porphyrin-peptide-folate (PPF) probe developed previously as folate receptor (FR) targeted fluorescent/PDT agent, and evaluated the potential of turning the resulting 64Cu-PPF into a positron emission tomography (PET) probe for cancer imaging. Noninvasive PET imaging followed by radioassay evaluated the tumor accumulation, pharmacokinetics and biodistribution of 64Cu-PPF. 64Cu-PPF uptake in FR-positive tumors was visible on small-animal PET images with high tumor-to-muscle ratio (8.88 ± 3.60) observed after 24 h. Competitive blocking studies confirmed the FR-mediated tracer uptake by the tumor. The ease of efficient 64Cu-radiolabeling of PPF while retaining its favorable biodistribution, pharmacokinetics and selective tumor uptake, provides a robust strategy to transform tumor-targeted porphyrin-based photosensitizers into PET imaging probes.
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DOI：
10.1016/s0006-3061(00)80224-0
发表时间：
1975-01-01
期刊：
BIOINORGANIC CHEMISTRY
影响因子：
--
作者：
HAMBRIGHT, P;FAWWAZ, R;VALK, P
通讯作者：
VALK, P
影响因子：
56.9
作者：
WRENN, FR;GOOD, ML;HANDLER, P
通讯作者：
HANDLER, P
影响因子：
4.7
作者：
Stefflova, Klara;Li, Hui;Zheng, Gang
通讯作者：
Zheng, Gang
DOI：
10.1073/pnas.98.3.1206
发表时间：
2001-01-30
影响因子：
11.1
作者：
Lewis, JS;Laforest, R;Welch, MJ
通讯作者：
Welch, MJ
影响因子：
1.5
作者：
Soucy-Faulkner, Anton;Rousseau, Jacques A.;van Lier, Johan E.
通讯作者：
van Lier, Johan E.